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H. J. Chowdhery studies on the subfamily apostasioideae.. 1-13shodhganga.inflibnet.ac.in/bitstream/10603/81145/11/11... · 2018-07-07 · and Kim Guncheol. Synthesis of amide and

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REFERENCES

1. Family Welfare Statistics in India, Ministry of Health and Family Welfare,

Government of India. 2009 and www.tbcindia.org

2. Family Welfare Statistics in India, Ministry of Health and Family Welfare,

Government of India, 2009 and http://mohfw.nic.in/Final%20website/

Website%209,%20August%202009.htm

3. Family Welfare Statistics in India, Ministry of Health and Family Welfare,

Government of India, 2009 and http://mohfw.nic.in/NRHM/Documents/

Mission_Document.pdf

4. http://mohfw.nic.in/National_Leprosy_Eradication_Programme/curr_stats06.html

5. http://nvbdcp.gov.in/dengue6.html

6. http://nvbdcp.gov.in/Doc/Dengue-CD-December2010.pdf

7. http://www.textbookofbacteriology.net/resantimicrobial.html

8. David S Perlin. Ed. Antimicrobial Resistance in Developing Countries, Part 2.

Springer, 2010, pp 137 - 156.

9. Stanton Hon Lung Kok, Chung Hin Chui, Wing Sze Lam, Jien Chen, Fung Yi

Lau, Raymond Siu Ming Wong, Gregory Yin Ming Cheng, Paul Bo San Lai,

Thomas Wai Tong Leung, Michael Wing Yiu Yu, Johimy Cheuk On Tang and

Albert Sun Chi Chan. Synthesis and structure evaluation of a novel

cantharimide and its cytotoxicity on SK-Hep-1 hepatoma cells. Bioorg. Med

Chem.Lett. 2007; 17(5): 1155-1159.

10. Aiello S, Wells G, Stone EL, Kadri H, Bazzi R, Bell DR, Stevens MF,

Matthews CS, Bradshaw TD and Westwell AD Synthesis and biological

properties of benzothiazole, benzoxazole, and chromen-4-one analogues of the

potent antitumor agent 2-(3,4-dimethoxyphenyl)-5-fluorobenzothiazole. J Med

Chem. 2008; 51(16): 5135-9.

DEPARTMENT OF CHEMISTRY, KUVEMPU UNIVERSITY Page 194

REFERENCES

11. E. Stone, R. Bazzi, D. Bell, C.S. Matthews, R. Singh, P.B. Farmer, A.M.

Burger, A.D. Westwell, M.F.G. Stevens and T.D. Bradshaw. Aryl

hydrocarbon receptor ligands 2-(3,4-dimethoxyphenyl)-fluorobenzothiazoles

elicit potent and selective in vitro antitumor activity, inducing DNA damage

that is independent of CYPlAl bioactivation. Eur. J. Cancer Suppl. 2006;

4(12): 96.

12. Masao Yoshida, Ichiro Hayakawa, Noriyuki Hayashi, Toshinori Agatsuma,

Youko Oda, Fumie Tanzawa, Shiho Iwasaki, Kumiko Koyama, Hidehiko

Furukawa, Shinichi Kurakata and Yuichi Sugano. Synthesis and biological

evaluation of benzothiazole derivatives as potent antitumor agents. Bioorg.

Med. Chem.Lett. 2005; 15(14): 3328-3332.

13. T. Bradshaw, C. Leong, M. Suggitt, D. Swaine, M. Bibby and M. Stevens. In

vitro, in vivo and in silico examination of the activity of antitumor 2-(4-

amino-3-methylphenyl)-5-fluorobenzothiazoles. Eur. J. Cancer Suppl. 2004;

2(8): 20

14. Ian Hutchinson, Tracey D. Bradshaw, Charles S. Matthews, Malcolm F. G.

Stevens and Andrew D. Westwell. Antitumour benzothiazoles. Part 20: 3'-

Cyano and 3'-Alkynyl-Substituted 2-(4'-Aminophenyl benzothiazoles as new

potent and selective analogues. Bioorg. Med. Chem. Lett. 2003; 13(3): 471-

474.

15. Michael S Christodoulou, Francesco Colombo, Daniele Passarella, Gabriella

leronimo, Valentina Zuco Michelandrea De Cesare and Franco Zunino.

Synthesis and biological evaluation of imidazolo[2,l-6]benzothiazole

derivatives, as potential p53 inhibitors. Bioorg. Med. Chem. 2011; 19(5):

1649-1657.

DEPARTMENT OF CHEMISTRY, KUVEMPU UNIVERSITY Page 195

REFERENCES

16. Hemal A. Bhuva and Suvarna G. Kini. Synthesis, anticancer activity and

docking of some substituted benzothiazoles as tyrosine kinase inhibitors.

Journal of Molecular Graphics and Modelling. 2010; 29(1); 32-37.

17. Catriona G. Mortimer, Geoffrey Wells, Jean-Philippe Crochard, Erica L.

Stone, Tracey D. Bradshaw, Malcohn F. G. Stevens, and Andrew D.

Westwell. Antitumor Benzothiazoles. 2-(3,4-Dimethoxyphenyl)-5-

fluorobenzothiazole (GW 610, NSC 721648), a Simple Fluorinated 2-

Arylbenzothiazole, Shows Potent and Selective Inhibitory Activity against

Lung, Colon, and Breast Cancer Cell Lines. J. Med. Chem. 2006; 49 (1): 179-

185

18. Song Eun Young , Kaur Navneet, Mi-Young Park , Jin Yinglan , Lee Kyeong

and Kim Guncheol. Synthesis of amide and urea derivatives of benzothiazole

as Raf-1 inhibitor. Eur. J. Med Chem. 2008; 43: 1519-1524.

19. Choi Suk-June, Park Hyen Joo, Sang Kook Lee, Sang Woong Kim, Gyoonhee

Han and Hea-Young Park Choo. Solid phase combinatorial synthesis of

benzothiazoles and evaluation of topoisomerase II inhibitory activity. Bioorg.

Med Chem. Lett. 2006; 14: 1229-1235.

20. Cedric J. Lion, Charles S. Matthews, Geoffrey Wells, Tracey D Bradshaw,

Malcolm FG Stevens and Andrew D Westwell. Antitumor properties of

fluorinated benzothiazole-substituted hydroxycyclohexa-2,5-dienones

Cquinoles'). Bioorg. Med. Chem. Lett. 2006; 16: 5005-5008.

21. Tzanopoulou Stamatia, loannis C. Pirmettis, George Patsis, Maria Paravatou-

Petsotas, Evangelia Livaniou and Minas Papadopoulos. Synthesis,

characterization and biological evaluation of M(I)(C0)3(NN0) complexes

(M=Re,^^"'Tc) conjugated to 2-(4-aminophenyl)benzothiazole as potential

breast cancer radiopharmaceuticals. J. Med. Chem.2006; 49: 5408-5410.

22. Raisa da R. Reis, Elisa C. Azevedo, Maria Cecilia B.V. de Souza, Vitor

Francisco Ferreira, Raquel C. Montenegro, Ana Jersia Araiijo, Claudia Pessoa,

DEPARTMENT OF CHEMISTRY, KUVEMPU UNIVERSITY Page 196

REFERENCES

Leticia V. Costa-Lotufo, Manoel O. de Moraes, Jose D.B.M. Filho, Alessandra

M.T. de Souza, Natasha C. de Carvalho, Helena C. Castro, Carlos R.

Rodrigues, Thatyana and R.A. Vasconcelos. Synthesis and anticancer

activities of some novel 2-(benzo[d]thiazol-2-yl)-8-substituted-2H-

pyrazolo[4,3-c]quinolin-3(5H)-ones. £Mn J. Med. Chem. 2011; 46(4): 1448-

1452.

23. Bradshaw T D and Westwell A D. Curr. Med. Chem. 2004; 11: 1241-1253.

24. Bradshaw T D, Trapani V, Vasselin D A and Westwell A D. Current Pharm

Design 2002; 8: 2475-2590.

25. Patterson L H and Murray G E. Current Pharm Design 2002; 8: 1335-1347.

26. Hutchinson I, Chua M, Bradshaw T D, Stevens F G and Westwell A D. J.

Med Chem.imi; 44: 1446-1455.

27. Zhao Wang, Xuan-Hong Shi, Jia Wang, Tian Zhou, You-Zhi Xu,Ting-

Ting Huang, Yan-Fang Li, Ying-Lan Zhao, Li Yang,Sheng-Yong Yang, Luo-

Ting Yu and Yu-Quan Wei Synthesis, structure-activity relationships and

preliminary antitumor evaluation of benzothiazole-2-thiol derivatives as novel

apoptosis inducers. Bioorg. Med. Chem. Lett, 2011; 21(4): 1097-1101.

28. Wan-Ping Hu, Yin-Kai Chen, Chao-Cheng Liao, Hsin-Su Yu, Yi-in Tsai, Shu-

Mei Huang, Feng-Yuan Tsai, Ho-Chuan Shen, Long-Sen Chang and Jeh-

Jeng Wang. Synthesis, and biological evaluation of 2-(4aminophenyl)

benzothiazole derivatives as photosensitizing agents. Bioorg. Med Chem.,

2010; 18(16; .-6197-6207.

29. V. Raja Solomon, Changkun Hu and Hoyun Lee. Hybrid pharmacophore

design and synthesis of isatin-benzothiazole analogs for their anti-breast

cancer activity. 5ioorg. Med. Chem., 2009; 17(21);7585-7592.

DEPARTMENT OF CHEMISTRY, KUVEMPU UNIVERSITY Page 197

REFERENCES

30. Weijun Xu, Gang Chen, Weiliang Zhu and Zhili Zuo. Molecular docking and

structure-activity relationship studies on benzothiazole based non-peptidic

BACE-1 inhibitors. Bioorg. Med. Chem. Lett., 2010; 20(21): 6203-6207.

31. Taleb H. Al-Te, Raed A. Al-Qawasmeh and Rania Zaarour. Design, synthesis

and m vi>o antimicrobial evaluation of novel Imidazo[l,2-a]pyridine and

imidazo[2,l-6][l,3] benzothiazole motifs. Eur. J. Med. Chem. Article in press.

doi:10.1016/j.ejmech.2011.02.051.

32. Samir Bondock, Walid Fadaly and Mohamed A. Metwally. Enaminonitrile in

heterocyclic synthesis: Synthesis and antimicrobial evaluation of some new

pyrazole, isoxazole and pyrimidine derivatives incorporating a benzothiazole

moiety. Eur. J. Med Chem., 2009; 44(12): 4813-4818.

33. Sohail Saeed, Naghmana Rashid, Peter G. Jones, Muhammad Ali, Rizwan

Hussain. Synthesis, characterization and biological evaluation of some

thiourea derivatives bearing benzothiazole moiety as potential antimicrobial

and anticancer agents. Eur. J. Med. Chem., 2010; 45: 1323-1331.

34. Nargund L V G, Sreenivasa Murthy V, Jayachandran E and Shivakumar B.

Anthelmintic activity of 8-Fluro-9-substitued (l,3)-Benzothialzolo (5, 1-6)-

1,3,4-Triazoles on Perituma Posthuma. Indian drugs 1999; 36(2): 137-139.

35. Pattan Shashikant R, Khade Amol, Pawar P D, Taranalli A D, Kittur B S and

Borkar S D. Synthesis of 2-amino [5'-(4-sulphonyl benzylidene)-2,4-

thiazolidinedione]-6-fluorobenzothiazoles as anti-inflammatory agents. Ind. J.

Het. Chem. 2007; 16: 299-300.

36. Oldrich Pytela and Vera klimeasova. Effect of substitution on the

antimycobacterial activity of 2-(Substituted benzyl) sulfanyl benzimidazoles,

benzothiazoles and benzoxazoles- A QSAR study. Chem.Pharm.Bull. 2011;

59(2): 179- 184.

DEPARTMENT OF CHEMISTRY, KUVEMPU UNIVERSITY Page 198

REFERENCES

37. Ivica Sigmundova, Pavol Zahradnik, Peter Magdolen and Helena Bujdakova.

Synthesis and study of new antimicrobial benzothiazoles substituted on

heterocyclic ring. ARKIVOC. 2008: 183 - 192.

38. Balram Soni, Mahendra Singh Ranawat, Rambabu Sharma, Anil Bhandari and

Sanjay Sharma. Synthesis and evaluation of some new benzothiazole

derivatives as potential antimicrobial agents. Eur. J. Med.

Chem., 2010; 45(7):293S - 2942.

39. Samir Bondock, Walid Fadaly and Mohamed A. Metwally. Synthesis and

antimicrobial activity of some new thiazole, thiophene and pyrazole

derivatives containing benzothiazole moiety. Eur. J. Med Chem.,

2010; ^5rP;:3692-3701.

40. Hipparagi SM, Majumder UK, Parikshit B, Geethavani M and Suresh Kumar

V. Microwave assisted Synthesis and antimicrobial activity of 7-chloro-6-

fluoro-2-(substituted aromatic sulphonyl hydrazino)benzothiazoles. Oriental

Journal of Chemistry 2007; 23(2): 665-668.

41. Hipparagi S M., Majumder U K, Kanchan Soni, Vyavahare Manoj, Panpaliya

Prashant and Nargund L V G. Synthesis and antimicrobial activity of 7-

substituted-2-(3,5-dimethyl-pyrazol-1 -yl)-6-fluoro-2,3-dihydro-

benzothiazoles. OrientalJoumal of Chemistry 2006; 22(3): 613-616.

42. Aravind M Badiger. Design and synthesis of heterocyclic compounds of

biological interest. Ph.D thesis, 2006. Kuvempu University, Shimoga, India.

42A. Joel G Hardman and Lee E Limbird (eds), in Goodman and Gilman's The

Pharmacological Basis of Therapeutics. 10* edition 2001. Mc.Graw Hill, New

York. Chapter 26.

43. R. Paramashivappa, P. Phani Kumar, P. V. Subba Rao and A. Srinivasa Rao.

Design, synthesis and biological evaluation of benzimidazole/benzothiazole

and benzoxazole derivatives as cyclooxygenase inhibitors. Bioorg. Med Chem.

Lett., 2003; 13(4): 657-660.

DEPARTMENT OF CHEMISTRY, KUVEMPU UNIVERSITY Page 199

REFERENCES

44. Guo Hua Jin, Hua Li, Semi An, Jae-Ha Ryu and Raok Jeon. Design, synthesis

and activity of benzothiazole-based inhibitors ofNOproduction inLPS-

activated macrophages. Bioorg. Med. Chem. Lett., 2010; 20(21): 6199-6202.

45. Athina A. Geronikaki, Alexey A. Lagunin, Dimitra I. Hadjipavlou-Litina,

Phaedra T. Eleftheriou, Dmitrii A. Filimonov, Vladimir V. Poroikov, Intekhab

Alam and Anil K. Saxena. Computer-Aided Discovery of Anti-Inflammatory

ThiazoHdinones with Dual Cyclooxygenase/Lipoxygenase Inhibition. J. Med.

Chem., 2008; 51(6): 1601-1609

46. Nilgiin Karali, Ozlen Giizel, Nurten Ozsoy, Suheyla Ozbey and Aydm

Salman. Synthesis of new spiroindolinones incorporating a benzothiazole

moiety as antioxidant agents. Eur. J. Med. Chem., 2010; 45(3): 1068 - 1077.

47. Ming-Qiang Zheng, Duan-Zhi Yin, Jin-Ping Qiao, Lan Zhang and Yong-Xian

Wang. Syntheses and evaluation of fluorinated benzothiazole anilines as

potential tracers for P-amyloid plaques in Alzheimer's disease. J. Fluorine

Chem. 2008; 129(3): 210-216.

48. K. Serdons, T. Verduyckt, D. Vanderghinste, J. Cleynhens, P. Borghgraef, P.

Vermaelen, C. Terwinghe, F. Van Leuven, K. Van Laere, H. Kung, G.

Bormans and A. Verbruggen. Synthesis of'^F-labelled 2-(4'-fluorophenyl)-

1,3-benzothiazole and evaluation as amyloid imaging agent in comparison

with ['^C]PIB.. Bioorg. Med Chem.Lett., 2009; 19(3): 602-605.

49. Serdons K, Verduyckt T, Cleynhens J, Terwinghe C, Mortelmans L and

Bormans G. Synthesis and evaluation of a ^̂ "̂ Tc-BAT-phenylbenzothiazole

conjugate as a potential in vivo tracer for visualization of amyloid p. Bioorg.

Med Chem. Lett. 2007; 17: 6086-6090.

50. Masahiro Ono, Shun Hayashi, Hiroyuki Kimura, Hidekazu Kawashima, Morio

Nakayama and Hideo Saji._Push-pull benzothiazole derivatives as probes for

detecting P-amyloid plaques in Alzheimer's brains. Bioorg. Med. Chem.,

2010; 17(19): 7002-7007.

DEPARTMENT OF CHEMISTRY, KUVEMPU UNIVERSITY Page 200

REFERENCES

51. Xie Yuli, Deng Shixian, Zhenzhang Chen, Shidu Yan and Donald W. Landry,

Identification of small-molecule inhibitors of the Ap-ABAD interaction.

Bioorg. Med. Chem. Lett. 2006; 16: 4657-4660.

52. Xiangji Chen, Pingrong Yu, Lianfeng Zhang and Boli Liu, Synthesis and

biological evaluation of ^̂ ""Tc, Re-monoamine-monoamide conjugated to 2-(4-

aminophenyl) benzothiazole as potential probes for p-amyloid plaques in the

brain. Bioorg. Med. Chem. Lett. 2008; 18: 1442-1445.

53. J. Benavides, J. C. Camelin, N. Mitrani, F. Flamand, A. Uzan, J-J. Legrand,

C. Gueremy and G. Le Fur. 2-Amino-6-trifluoromethoxy benzothiazole, a

possible antagonist of excitatory amino acid neurotransmission—^11 :

Biochemical properties. A^ewrop/zarwaco/ogy, 1985; 24(11): 1085-1092.

54. Rana A, Siddiqui N, Khan S A, Haque S E and Bhat M S. iV-{[(6-Substituted-

l,3-benzothiazole-2-yl)amino]carbonothioyl}-2/4-substituted benzamides:

Synthesis and pharmacological evaluation. Eur. J. Med. Chem. 2008; 43(5):

114-1122

55. Heiser V, Engemann S, Brocker W, Dunkel I, Boeddrich A, Waelter S,

Nordhoff E, Lurz R, Schugardt N, Rautenberg S, Herhaus C, Barnickel G,

Bottcher H, Lehrach H and Wanker EE. Identification of benzothiazoles as

potential polyglutamine aggregation inhibitors of Huntington's disease by

using an automated filter retardation assay. Proc Natl. Acad. Sci. USA. 2002;

99Suppl4: 16400-16406.

56. Emma Hockly, Jamie Tse, Amy L. Barker,

DonnaL. Moolman,JeanLuc Beunard, AdrianP. Revington, Kim Holt, Sunny S

unshine,Hilary Moffitt, Kirupa Sathasivam, Benjamin Woodman, Erich

E. Wanker, Philip A.S. Lowden and Gillian P. Bates. Evaluation of the

benzothiazole aggregation inhibitors riluzole and PGL-135 as therapeutics for

Huntington's disease. Neurobiology of Disease, 2006; 21(1).- 228-236.

DEPARTMENT OF CHEMISTRY, KUVEMPU UNIVERSITY Page 201

REFERENCES

57. Tsutomu Araki,Yasuko Muramatsu, Katsuyuki Tanaka, Mitsunobu Matsubara

andYutaka Imai. Riluzole (2-amino-6-trifluoromethoxy benzothiazole)

attenuates MPTP (l-methyl-4-phenyl-l,2,3,6-tetrahydropyridine)

neurotoxicity in mice. Neuroscience Letters, 2001; 312(1).- 50-54.

58. Chi B. Vu, Jill C. Milne, David P. Carney, Jeffrey Song, Wendy Choy, Philip

D. Lambert,DavidJ. Gagne, Michael Hirsch,Angela Cote, Meghan Davis, Elde

n Lainez, Nekeya Meade, Karl Normington, Michael R. Jirousek and Robert

B. Pemi. Discovery of benzothiazole derivatives as efficacious and enterocyte-

specificMTP inhibitors, fl/oorg. Med. Chem. Lett., 2009; 19(5): 1416-1420.

59. Hiroki Fujieda, Shinya Usui, Takayoshi Suzuki, Hidehiko Nakagawa,Michitak

a Ogura, Makoto Makishima and Naoki Miyata. Phenylpropanoic acid

derivatives bearing a benzothiazole ring as PPAR5-selective agonists. Bioorg.

Med. Chem. Lett. 2007; 17(15): 4351-4357.

60. Liu C, Lin J, Pitt S, Zhang RF, Sack JS, Kiefer SE, Kish K, Doweyko AM,

Zhang H, Marathe PH, Trzaskos J, Mckinnon M, Dodd JH, Barrish JC,

Schieven GL and Leftheris K. Benzothiazole based inhibitors of p38alpha

MAP kinase. Bioorg. Med Chem. Lett., 2008; 18(6): 1874-1879.

61. K. Rehse, T. Ciborski and E. Ltidtke. P67 benzothiazole-2(3H)-nitrosimines -

new no-donors with antiplatelet and antithrombotic activities. Eur. J. Pharm.

Sc., 1994;2(1-2):135.

62. Chunquan Sheng, Jie Zhu, Wannian Zhang, Min Zhang, Haitao Ji, Yunlong

Song, Hui Xu, Jianzhong Yao, Zhenyuan Miao, Youjun Zhou, Ju Zhu and

Jiaguo Lti. 3D-QSAR and molecular docking studies on benzothiazole

derivatives as Candida albicans A'-myristoyltransferase inhibitors. Eur. J.

Med Chem., 2007;42(4):477-486.

63. Shaikh A R, Ismael M, Del Carpio C A, Tsuboi H, Koyama M, Endou A,

Kubo M, Broclawik E and Miyamoto A. Three-dimensional quantitative

structure-activity relationship (3 D-QSAR) and docking studies on

DEPARTMENT OF CHEMISTRY, KUVEMPU UNIVERSITY Page 202

REFERENCES

(benzothiazoIe-2-yl) acetonitrile derivatives as c-Jun N-terminal kinase-3

(JNK3) inhibitors. Bioorg. Med. Chem. Lett., 2006; 16(22): 5917-5925.

64. Chunquan Sheng, Jie Zhu, Wannian Zhang, Min Zhang, Haitao Ji and

Yunlong Song. 3D-QSAR and molecular docking studies on benzothiazole

derivatives as Candida albicans N-myristoyltransferase inhibitors. Eur. J. Med.

Chem. 2007; 42: 477-486.

65. Aravind M Badiger, Malleshappa N Noolvi and P.Vasudeva Nayak. QSAR

study of benzothiazole derivatives as p561ck inhibitors. Letters in Drug Design

and Discovery 2006; 3: 550 - 560.

66. Gupta R R, Kumar M, Gupta V, Eds., Heterocyclic chemistry Vol II, P'

edn, Springer Verlag.1999. pp 436-440.

67. Xian Huang and Jing Tang. Solid phase synthesis of benzothiazole and

thiophene derivatives based on resin-bound cyclic malonic acid ester.

Tetrahedron.. 2003; 59(26): 4851-4856.

68. Umesh R. Pratap, Jyotirling R. Mali, Dhanaji V. Jawale and Ramrao A. Mane.

Bakers' yeast catalyzed synthesis of benzothiazoles in an organic medium.

Tet. Lett. 2009; 50(12): 1352-1354.

69. Hideaki Hioki, Kimihito Matsushita, Miwa Kubo and Mitsuaki Kodama.

Combinatorial Synthesis of Benzothiazoles and Benzimidazoles Using a

Trace less Aniline Linker. Journal of Combinatorial Chemistry 2006, 8 (4):

462^63.

70. Asit K Chakraborti, Rudrawar S, Sharma L and Kaur G. An efficient

conversion of phenolic esters to benzothiazoles under mild and virtually

neutral conditions. Synlett 2004: 1533-1536.

71. Asit K Chakraborti, Selvam C, Kaur G and Shrikant Bhagat. An efficient

synthesis of benzothiazoles by direct condensation of carboxylic acids with 2-

amino thiophenol under microwave irradiation. Synlett 2004: 0851-0855.

DEPARTMENT OF CHEMISTRY, KUVEMPU UNIVERSITY Page 203

REFERENCES

72. Dawei Ma, Xu Lu, Liu Shi, Hui Zhang, Yongwen Jiang and Xiangqian Liu.

Angew. Chem. Int. Edn. 2005; 50(5):1118-112L

73. Gavin W. Stewart, Carl A. Baxter, Ed Cleator and Faye J. Sheen. A Mild and

Efficient One-Pot Synthesis of 2-Aminated Benzoxazoles and Benzothiazoles.

J. Org. Chem. 2009; 74 (8): 3229-3231.

74. D. Subhas Bose and Mohd. Idrees. Metal-Free Cascade Intramolecular 5-

Arylation: Regioselective Synthesis of Substituted Benzothiazoles. J. Org.

Chem., Article ASAP. (DOI: 10.1021/jo802826x)

75. Castagnolo D, De Logu A, Marco Radi, Bechi B, Manetti F, Magnani M,

Supino S, Chisu R L and Botta M. Synthesis, biological evaluation and SAR

study of novel pyrazole analogues as inhibitors of Mycobacterium

tuberculosis. Bioorg. Med. Chem. Lett., 2008; 16(18): 8587-8591.

76. Castagnolo D, De Logu A, Marco Radi, Bechi B, Manetti F, Pagano M,

Supino S, Rita M, Saddi M and Botta M. Synthesis, biological evaluation, and

SAR study of novel pyrazole analogues as inhibitors of Mycobacterium

tuberculosis: Part 2. Synthesis of rigid pyrazolones. Bioorg. Med. Chem., In

Press, Corrected Proof, Available online 29 May 2009.

11. David A C, George P, Ben K, James D and Don G. synthesis of insecticidal

fluorinated anthranilic diamides. Bioorg. Med. Chem. Lett. 2008; 16: 3163 -

3170.

78. Samir Bondock, Ramy Rabie, Hassan A. Etman and Ahmed A. Fadda.

Synthesis and antimicrobial activity of some new heterocycles incorporating

antipyrine moiety. Eur. J. Med. Chem., 2008;43(10):2122-2129

79. Bantwal Shivarama Holla, Manjathuru Mahalinga, Mari Sitambaram

Karthikeyan, Padiyath Mohamed Akberali and Nalilu Sucheta Shetty.

Synthesis of some novel pyrazolo[3,4-fi(]pyrimidine derivatives as potential

antimicrobial agents. Bioorg. Med. Chem, 2006; 14(6):2040-2047

DEPARTMENT OF CHEMISTRY, KUVEMPU UNIVERSITY Page 204

REFERENCES

80. Mari Sithambaram Karthikeyan, Bantwal Shivarama Holla and Nalilu

Suchetha Kumar. Synthesis and antimicrobial studies on novel chloro-fluorine

containing hydroxy pyrazolines. Eur. J. Med. Chem., 2007;42(l):30-36.

81. Flora F. Barsoum, Hanaa M. Hosni, Adel S. Girgis. Novel bis(l-acyl-2-

pyrazolines) of potential anti-inflammatory and moUuscicidal properties. .

Bioorg. Med. Chem.., 2006; 14(lI):3929-3937.

82. Subas M. Sakya, Kristin M. Lundy DeMello, Martha L. Minich, Bryson Rast,

Andrei Shavnya, Robert J. Rafka, et al. 5-Heteroatom substituted pyrazoles as

canine COX-2 inhibitors. Part 1: Structure-activity relationship studies of 5-

alkylamino pyrazoles and discovery of a potent, selective, and orally active

analog. Bioorg. Med Chem. Lett., 2006; 16(2): 288-292.

83. Nesrin G6khan-Kelek9i, Samiye Yabanoglu, Esra Kiipeli, Umut Salgin, Ozen

Ozgen, Giilberk U9ar, Erdem Ye§ilada, Engin Kendi, Akgul Ye§ilada, A. and

Altan Bilgin. A new therapeutic approach in Alzheimer disease: Some novel

pyrazole derivatives as dual MAO-B inhibitors and antiinflammatory

analgesics. Bioorg. Med Chem. 2007; 15(17): 5775 - 5786.

84. Hengmiao Cheng, Kristin M. Lundy DeMello, Jin Li, Subas M. Sakya, Kazuo

Ando, K. Kawamura, Tomoki Kato, Robert J. Rafka, Burton H. Jaynes, Carl

B. Ziegler, Rod Stevens, Lisa A. Lund, Donald W. Mann, Carolyn Kilroy,

Michelle L. Haven, Erik L. Nimz, Jason K. Dutra, Chao Li, Martha L. Minich,

Nicole L. Kolosko, et al. Synthesis and SAR of heteroaryl-phenyl-substituted

pyrazole derivatives as highly selective and potent canine COX-2

inhibitors Bioorg. Med. Chem. Lett., 2006; 16(8): 2076 - 2080.

85. Aldo Balsamo, Isabella Coletta, Angelo Gughelmotti, Carla Landolfi,

Francesca Mancini, Adriano Martinelli, Claudio Milanese, Filippo Minutolo,

Susanna Nencetti, Elisabetta Orlandini, Mario Pinza, Simona Rapposelli and

Armando Rossello. Synthesis of heteroaromatic analogues of (2-aryl-l-

cyclopentenyl-l-alkylidene)-(arylmethyloxy)amine COX-2 inhibitors: effects

on the inhibitory activity of the replacement of the cyclopentene central core

DEPARTMENT OF CHEMISTRY, KUVEMPU UNIVERSITY Page 205

REFERENCES

with pyrazole, thiophene or isoxazole ring. Eur. J. Med Chem., 2003; 38(2):

157-168.

86. Menozzi G, Mosti L, Schenone P, D'Amico M, Falzarano C, Rossi F. N-

substituted 4-carboxy-l-phenyl-lH-pyrazole-5-propanamides with

antiinflammatory, analgesic, antipyretic and platelet antiaggregating activities.

IIFarmaco. 1993; 48(4): 539-549

87. Menozzi G, Mosti L, Schenone P, D'Amico M, Filippelli A and Rossi F. 4H-

thieno[3,4-c]pyrazole derivatives with antiinflammatory, analgesic, antipyretic

and platelet antiaggregating activities. 11 Farmaco. 1992; 47(12): 1495-511.

88. Menozzi G., Mosti L., Schenone P., D.Amico M., Falciani M. and Filippelli

W.l-Aryl-lH-pyrazole-5-acetic acids with anti-inflammatory, analgesic and

other activities.//Far/naco. 1994; 49(2): 115-9.

89. Farghaly A. M., Chaaban I., Khalil M. A. and Behkit A. A. Non-steroidal anti­

inflammatory agents, II: Synthesis of novel pyrazole and pyrazoline

derivatives of 4(3H)-quinazolinone. Arch. Pharm. (Weinheim). 1990; 323(5):

311-5.

90. Meena Patel V, Randy Bell, Sandra Majest and Rodger Henry. Synthesis of

4,5-diaryl-lH-pyrazole-3-ol derivatives as potential COX-2 inhibitors. J. Org.

Chem. 2004; 69(21):7058-65.

91. Ashish Kumar Tewari, Priyanka Srivastava, Ved Prakash Singh, Amit Singh,

Raj Kumar Goel and Chethampadi Gopi Mohan. Novel anti-inflammatory

compounds based on Pyrazole based dimeric compounds; Design, synthesis,

docking and in vivo activity. Chem .Pharm. Bull. 2010; 58(5): 634 - 638.

92. Babasaheb P Bandgar, Shrikant S Gawande, Ragini G Bodade, Nalini

M Gawande and Chandrahasya N Khobragade. Synthesis and biological

evaluation of a novel series of pyrazole chalcones as anti-inflammatory,

antioxidant and antimicrobial agents. Bioorg. Med. Chem. Lett., 2007; 17(24):

8168-8173.

DEPARTMENT OF CHEMISTRY, KUVEMPU UNIVERSITY Page 206

REFERENCES

93. Babasaheb P. Bandgar, Jalinder V Totre, Shrikant S Gawande, C N

Khobragade, Suchita C. Warangkar and Prasad D Kadam. Synthesis of novel

3,5-diaryl pyrazole derivatives using combinatorial chemistry as inhibitors of

tyrosinase as well as potent anticancer, anti-inflammatory agents. Bioorg.

Med Chem. Lett. 2008; 18(16): 6149-6155.

94. Mohy El-Din, Mahmoud M., Senbel, Amira M and Bistawroos, Azza A. A

novel COX-2 inhibitor pyrazole derivative proven effective as an anti­

inflammatory and analgesic drug. Basic & Clinical Pharmacology &

Toxicology IQl^; 107: 919-990.

95. Bekhit A A, Ashour H M, Bekhit Ael-D and Bekhit S A. Synthesis and

biological evaluation of novel pyrazole derivatives as anti-inflammatory

antimicrobial agents. Med. Chem. 2009; 5(2;.-103-17.

96. Takehiro Ochi, Katsue Jobomagari, Atsuo Yonezawa, Kanae Matsumori and T

Takashi Fujii. Anti-inflammatory and analgesic effects of a novel pyrazole

derivative, FR140423. Eur.J. Pharmacol. 1999; 365(2-3): 259-266.

97. Tsuji K, Konishi N, Spears GW, Ogino T, Nakamura K, Tojo T, Ochi

T, Shimojo F, Senoh H and Matsuo M. Studies on anti-inflammatory agents.

V. Synthesis and pharmacological properties of 3-(difluoromethyl)-l-(4-

methoxyphenyl)-5- [4-(methylsulfmyl)phenyl]pyrazole and related

compounds. Chem. Pharm. Bull. 1997; 45(9): 1475-81.

98. Joanne M. Smallheer, Richard S. Alexander, Jianmin Wang, Shuaige Wang,

Suanne Nakajima, Karen A. Rossi, Angela Smallwood, Frank Barbera, Debra

Burdick, Joseph M. Luettgen, Robert M. Knabb, Ruth R. Wexler and

Prabhakar K. Jadhav. SAR and factor IXa crystal structure of a dual inhibitor

of factors IXa and Xa. Bioorg. Med Chem. Lett., 2004; 14(21): 5263-5267.

99. Ryan P. Wurz, Liping H. Pettus, Shimin Xu, Bradley Henkle, Lisa Sherman,

Matthew Plant, Kent Miner, Helen McBride, Lu Min Wong, Christiaan J.M.

Saris, Matthew R. Lee, Samer Chmait, Christopher Mohr, Faye Hsieh and

DEPARTMENT OF CHEMISTRY, KUVEMPU UNIVERSITY Page 207

REFERENCES

Andrew S. Tasker. Part 1: Structure-Activity Relationship (SAR)

investigations of fused pyrazoles as potent, selective and orally available

inhibitors of p38a mitogen-activated protein kinase. Bioorg. Med. Chem. Lett.,

2010; 20 (5): 1680-1684.

100. Alan X. Wang, Qinghua Xie, Ben Lane, Karl W. MoUison, Gin C. Hsieh,

Kennan Marsh, Michael P. Sheets, Jay R. Luly and Michael J. Coghlan.

Synthesis and immunosuppressant activity of pyrazole carboxamides. Bioorg.

Med. Chem. Lett, 1998; 8(19): 2787-2792.

101. Kenneth L. Kirk. Fluorine in Medicinal Chemistry: recent therapeutic

applications of fluorinated small molecules. J. Fluorine Chem. 2006; 127(2):

1013-1029.

102. Andrei A Gakh and Michael N Burnett. Extreme Modulation Properties of

aromatic fluorine. J. Fluorine Chem. 2011; 132: 88 - 93

103. R. Peters, in: Proceedings of the Ciba Foundation Symposium on Carbon-

Fluorine Compounds: Chemistry, Biochemistry, and Biological Activities,

Elsevier, Amsterdam, 1972: pp. 55-76.

104. J. Fried, and E.F. Sabo. J. Am. Chem. Soc.1953; 75: 2273-2274.

105. C. Heidelberger, N.K. Chaudhuri, P. Danneberg, D. Mooren, L. Greisbach, R.

Duschinsky, R.J. Scnnitzer, E. Pleaven and J.Scheiner. Nature 1957; 179:

663-666.

106. A.I. Vogel, A.R. Tatchell, B.S. Fumis, A.J. Hannaford, P.W.G. Smith. Vogel's

Textbook of Practical Organic Chemistry,5th Edition. 1996, Prentice Hall.

107. Sreenivas Murthy V, A N Nagappa and L V G Nargund. Synthesis of 8-

fluoro-9-substituted (1,3) benzothiazolo (5,1-b) -1,2,4- triazoles as antifungal

agents. Ind. J. Het. Chem. 1998; 8: 23-26.

108. James Lindley. Tetrahedron report number 163 : Copper assisted nucleophilic

substitution of aryl halogen. Tetrahedron 1984; 40(9): 1433-1456.

109. Hanhui Xu and Christian Wolf Copper catalyzed coupling of aryl chlorides

bromides and iodides with amines and amides. Chem. Comm. 2009: 1715 -

1717.

DEPARTMENT OF CHEMISTRY, KUVEMPU UNIVERSITY Page 208

REFERENCES

109A. Jerry March. Advanced Organic Chemistry, 3"* edition. Wiley Eastern Limited.

1994: chapter 6

110. William Kemp in Organic Spectroscopy. Macmillan press, London 1991.

Chapter 3.

111. Subhash Chandra Parija. Textbook of Practical Microbiology, le, 2007. Ahuja

Publishing House, New Delhi: pp 92 - 94.

112. K R Aneja. Experiments in microbiology plant pathology tissue culture and

mushroom production technology, 3e. New Age International (P) ltd. New

Delhi: pp 556.

113. Bente L. Halvorsen, Kari Holte, Mari C. W. Myhrstad, Ingrid Barikmo, Erlend

Hvattum, Siv Fagertun Remberg, Anne-Brit Wold, Karin Haffoer and Halvard

Baugerod, Lene Frost Andersen, Moskaug, David R. Jacobs, Jr. and Rune

Blomhoff. A Systematic Screening of Total Antioxidants in Dietary Plants.

Journal of Nutrition. 2002; 132: 461-471.

114. Mruthyunjaya K. Phytochemical and pharmacological screening of some

herbs used in folk medicine for their hepatoprotective and antoxidant activity.

Ph.D thesis: Rajiv Gandhi University of Health Sciences, Karnataka.

September 2008.

115. Dey N C, Debashish Sinha and P K Dey.eds, Text Book of Pathology. New

central book agency (Pvt) ltd. Calcutta 2"'' edn.; 1995: pp 6.1 - 6.59.

116. H P Rang, M M Dale, J M Ritter and P K Moore. Eds, in Pharmacology.

Churchill livingstone.5* edn.; 2003: pp 26 - 29.

117. L. V. G. Nargund, G. R. N. Reddy and V. Hariprasad. Anti-inflammatory

activity of substituted 1,3,4-Oxadiazoles. Journal of Pharmaceutical Sciences.

1994; 83(2): 246-248.

118. Indian Pharmacopoeia. 3'̂ '' edition, Govt, of India. 1985: A-145.

119. Sheth U K, Dadkar N K, Kamat U G.eds in Selected topics in Experimental

Pharmacology. 1987, pp 21-230.

120. S K Kulkarni, Ed. Hand book of experimental pharmacology, 4e.Vallabhai

Prakashan, New Delhi, 2004. pp 128-130.

DEPARTMENT OF CHEMISTRY, KUVEMPU UNIVERSITY Page 209

REFERENCES

121. Crum-Brown C A and Eraser T R. On the connection between chemical

constitution and physiological action I. On the physiological action of the

salts of the ammonium bases derived from trichina. Trans. R. Soc. Edinburgh.

1868; 25: 151-203.

122. Mayer H. Lipoid theorie der narcose. Exp. Path. Pharm. 1899; 42:109-18.

123. Hansch C, Leo A and Taft. R W. A survey of Hammett substituent constants

and resonance and field parameters. Chem. Rev.\99\; 91: 165-195

124. Hansch C and Fujita T. The correlation of biological activity of plant growth

regulators and Chloromycetin derivatives with Hammett constants and

partition coefficients. J. Am. Chem.Soc. 1963; 85: 2817-2824.

125. Hansch C and Fujita T. p-a-7i Analysis: A method for the correlation of

biological and chemical structure. J. Am. Chem. Soc. 1964; 86: 1616-1626.

126. Hansch, C and Fujita T. A new substituent constant, 7t, derived from partition

coefficients. J. Am. Chem. Soc. 1964; 86: 5175-5180.

127. Hansch C. A quantitative approach to biochemical structure-activity

relationship. Act. Chem Res. 1969; 2: 232-239.

128. Hansch C and Fujita T. Synthesis and QSAR of some pyrrolo [2,1-a]

isoquinolines. J. Med Chem. 1968; 12: 766.

129. Hansch C. The QSAR paradigm in the design of less toxic molecules. Drug

Metab. Rev. 1984-85; 15: 1279-1294.

130. Free S M and Wilson, J W. A mathematical contribution to structure -activity

studies. J. Med Chem. 1964; 7: 395-399.

131. Hansch C, Garg R and Kurup A. Chembioinformatics and QSAR: A review of

QSAR lacking positive hydrophobic terms. Chem.Rev. 2001; 101: 619 - 672.

132. Kubiniyi H and Wolf M.(Eds) in Burgers Medicinal Chemistry and Drug

Discovery. New York. 1995: pp 497.

133. Martin Y C. Quantitative Drug Design, a critical introduction. Medicinal

Research Series, Volume 8. Marcel Dekker, New York 1978: pp.678-688.

134. Martin Y C and Holland J B. Discriminant Analysis of the relation between

physical properties and the inhibition of mono amine oxidase by amino

tetrahnes and amino indans. J. Med. Chem. 1974; 17:409-413.

DEPARTMENT OF CHEMISTRY, KUVEMPU UNIVERSITY Page 210

REFERENCES

135. Henry D R and Block. J H. Classification of Drugs by Discriminant Analysis

using Fragmnt Molecular Connectivity Values. J. Med. Chem. 1979; 22: 465-

472.

136. Hodentt. E M. Discriminant Analysis and Structure Activity Relatioship of 1-

naphtoquinones. J. Med. Chem. 1978; 21: 369-374.

137. Mc Farland J W and Cans D J. On the significance of clusters in the graphical

display of structure activity data. J. Med. Chem. 1986; 29: 505-514.

138. Kubinyi H. Quantitative Structure Activity Relationships: A mixed approach

based on Hansch and Free-Wilson Analysis. J. Med. Chem. 1976; 19: 587-

600.

139. Rogers D and Hopfinger A J. Application of Genetic Function Approximation

to QSAR and QSPR. J. Chem. Inf. Comput. Sci. 1994; 34: 854-866.

140. Kowar T R. Genetic Function Approximation experimental design: a new

method for experiemental design. J. Chem. Inf. Comput. Sci. 1998; 38: 858-

866.

141. Hansch C and Leo A. Partition coefficients and their uses. Chem. Rev. 1971;

71:525-616

142. Boyce C B C and Milborrow B V. A simple assessment of partition data for

correlating structure and biological activity using thin layer chromatography.

Nature 1965; 208: 537-539

143. Mirless M S, Mounlton S.J, Murphy C T and Taylor P J. Direct measurement

of octanol-water partition coefficients by high pressure liquid

chromatography. J. Med. Chem. 1976; 19: 615-619.

144. Blaney J M and Hansch C. Comprehensive Medicinal Chemistry: the rational

mechanistic study and therapeutic applications of chemical compounds.

Pergamon Press, Oxford 1990: pp495.

145. Sunil Kumar Singh, Saibaba Vobbalareddy, Srinivasa Rao Kalleda, Seshagiri

Rao Casturi, Srinivasa Raju Datla, Rao N.V.S. Mamidi, Ramesh Mullangi,

Rajagopalan Ramanujam, Koteswar Rao Yeleswarapu and Javed Iqbal.

Identification of 2-hydroxymethyl-4-[5-(4-methoxyphenyl)-3-trifluoromethyl-

pyrazoH-yl]-A^-propionylbenzenesulfonamide sodium as a potential COX-2

DEPARTMENT OF CHEMISTRY, KUVEMPU UNIVERSITY Page 211

REFERENCES

inhibitor for oral and parenteral administration. Bioorg. Med. Chem, 2006; 14:

8626 - 8634.

146. John H Block and John M Beale in Wilson and Gisvold's Textbook of

Organic Medicinal and Pharmaceutical Chemistry, l ie. Lippincott Williams

and Wilkins; 2004: Chapter 1

147. H P Rang, M M Dale, J M Ritter and P K Moore. Eds, in Pharmacology.

Churchill livingstone.S"' edn.; 2003: Chapter 2

148. Gehlhaar D K, Bouzida D and Rejto, P A. Proceedings of the Seventh

International Conference on Evolutionary Programming. 1998: 449.

149. Yang J M and Chen C C. Pwtew^ 2004; 55: 288.

DEPARTMENT OF CHEMISTRY, KUVEMPU UNIVERSITY Page 212