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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