Design and synthesis of sulfonyl-substituted 4,5-diarylthiazoles as selective cyclooxygenase-2 inhibitors

J S Carter; D J Rogier; M J Graneto; K Seibert; C M Koboldt; Y Zhang; J J Talley

doi:10.1016/s0960-894x(99)00158-4

Design and synthesis of sulfonyl-substituted 4,5-diarylthiazoles as selective cyclooxygenase-2 inhibitors

Bioorg Med Chem Lett. 1999 Apr 19;9(8):1167-70. doi: 10.1016/s0960-894x(99)00158-4.

Authors

J S Carter¹, D J Rogier, M J Graneto, K Seibert, C M Koboldt, Y Zhang, J J Talley

Affiliation

¹ G.D. Searle-Monsanto, St. Louis, MO 63198, USA.

PMID: 10328306
DOI: 10.1016/s0960-894x(99)00158-4

Abstract

A series of novel sulfone substituted 4,5-diarylthiazoles have been synthesized and evaluated for their inhibition of the two isoforms of human cyclooxygenase (COX-1 and COX-2). This series displays exceptionally selective COX-2 inhibition.

MeSH terms

Animals
Cyclooxygenase 2
Inhibitory Concentration 50
Isoenzymes / drug effects*
Prostaglandin-Endoperoxide Synthases / drug effects*
Rats
Sulfones / chemistry*
Thiazoles / chemical synthesis*

Substances

Isoenzymes
Sulfones
Thiazoles
Cyclooxygenase 2
Prostaglandin-Endoperoxide Synthases