A new series of selective COX-2 inhibitors: 5,6-diarylthiazolo[3,2-b][1,2,4]triazoles

Bioorganic and Medicinal Chemistry Letters

Volumn 7, Issue 1, 1997, Pages 57-62

  Roy, P ^a   Leblanc, Y ^a   Ball, R G ^b   Brideau, C ^a   Chan, C C ^a   Chauret, N ^a   Cromlish, W ^a   Ethier, D ^a   Gauthier, J Y ^a   Gordon, R ^a   Greig, G ^a   Guay, J ^a   Kargman, S ^a   Lau, C K ^a   O'Neill, G ^a   Silva, J ^a   Therien M ^a   Van Staden, C ^a   Wong, E ^a   Xu, L ^a   Prasit, P ^a   more..

^a MERCK FROSST CENTRE FOR THERAPEUTIC RESEARCH   (Canada)

^b MERCK RESEARCH LABORATORIES   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

5 BROMO 2 (4 FLUOROPHENYL) 3 (4 METHYLSULFONYLPHENYL)THIOPHENE; 6 (4 METHYLSULFONYLPHENYL) 5 PHENYLTHIAZOLO[3,2 B][1,2,4]TRIAZOLE; CYCLOOXYGENASE 1; CYCLOOXYGENASE 2 INHIBITOR; INDOMETACIN; ISOENZYME; NONSTEROID ANTIINFLAMMATORY AGENT; UNCLASSIFIED DRUG;

ANIMAL CELL; ANIMAL EXPERIMENT; ANIMAL MODEL; ANTIINFLAMMATORY ACTIVITY; ARTICLE; BIOAVAILABILITY; BLOOD; CHO CELL; CONTROLLED STUDY; DRUG SAFETY; DRUG SYNTHESIS; EDEMA; ENZYME INHIBITION; HUMAN; HUMAN TISSUE; IN VITRO STUDY; LIVER METABOLISM; LIVER MICROSOME; MONKEY; NONHUMAN; NORMAL HUMAN; NUCLEAR OVERHAUSER EFFECT; ORAL DRUG ADMINISTRATION; RAT; REACTION ANALYSIS; STEREOCHEMISTRY; STRUCTURE ACTIVITY RELATION; X RAY CRYSTALLOGRAPHY;

EID: 0343052955     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0960-894X(96)00582-3     Document Type: Article

References (12)

1. See preceding two papers.
2. Pignatello, R.; Mazzone, S.; Panico, A. M.; Mazzone, G.; Pennisi, G.; Castana, R.; Matera, M.; Blandino, G. Eur. J. Med. Chem. 1991, 26, 929.
3. Leblanc, Y.; Gauthier, J.-Y.; Ethier, D.; Guay, J.; Mancini, J.; Riendeau, D.; Tagari, P.; Vickers, P.; Wong, E.; Prasit, P. Bioorg. Med. Chem. Lett. 1995, 5, 2123.
4. Reitz, D. B.; Li, J. J.; Norton, M. B.; Reinhard, E. J.; Collins, J. T.; Anderson, G. D.; Gregory, S. A.; Kobolt, C. M.; Perkins, W. E.; Seibert, K.; Isakson, P. C. J. Med. Chem. 1994, 37, 3878.
5. Gans, K. R.; Gailbraith, W.; Roman, R. J.; Haber, S. B.; Kerr, J. S.; Schmidt, W. K.; Smith, C.; Hewes, W. E.; Ackerman, N. R.; J. Pharmacol. Exp. Ther. 1990, 254, 180.
6. Jones, R. G.; Ainsworth, C. J. Am. Chem. Soc. 1955, 77, 1538.
7. Haber, S. B. U. S. Patent 1989 4 820 827.
8. -3 and it has no chemical significance. The authors have deposited the atomic coordinates for this structure with the Cambridge Crystallographic Data Centre. The coordinates can be obtained on request from the Director, Cambridge Crystallographic Data Centre, 12 Union Road, Cambridge CB2 IEZ, UK. *Sheldrick, G.M., Acta Crystallogr. 1990, A46, 467-473. **Structure Determination Package Ver. 3, Enraf-Nonius, Delft, 1985.
9. Kargman, S.; Wong, E.; Greig, G.; Falgueyret, J.-P.; Cromlish, W.; Ethier, D.; Yergey, J.; Riendeau, D.; Evans, J.; Kennedy, B.: Tagari, P.; Francis, D.; O'Neill, G. P. Biochem. Pharmacol. 1996, 52, 1113.
10. Brideau, C.; Kargman, S.; Liu, S.; Dallob, A. L.; Ehrich, E. W.; Rodger, I. W.; Chan, C.-C. Inflamm. Res. 1996, 45, 68.
11. Chan, C.-C.; Black, C.; Boyce, S.; Brideau, C.; Ford-Hutchinson, A. W.; Gordon, R.; Guay, D.; Hill, R.; Li, C.-S.; Mancini, J.; Penneton, M.; Prasit, P.; Rasori, R.; Riendeau, D.; Roy, P.; Tagari, P.; Vickers, P.; Wong, E.; Rodger, I. W. J. Pharmacol. Exp. Ther. 1995, 274, 1531.
12. See preceding paper.