Synthesis and activity of sulfonamide-substituted 4,5-diaryl thiazoles as selective cyclooxygenase-2 inhibitors.

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Carter JS, Kramer S, Talley JJ, Penning T, Collins P, Graneto MJ, Seibert K, Koboldt CM, Masferrer J, Zweifel B

Synthesis and activity of sulfonamide-substituted 4,5-diaryl thiazoles as selective cyclooxygenase-2 inhibitors.

Bioorg Med Chem Lett. 1999 Apr 19;9(8):1171-4.

PubMed ID

10328307 [ View in PubMed

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Abstract

A series of sulfonamide-substituted 4,5-diarylthiazoles was prepared via three synthetic routes as selective COX-2 inhibitors. Recently in the synthesis of selective COX-2 inhibitors we have discovered that the sulfonamide moiety is a suitable replacement for the methylsulfonyl moiety yielding compounds with activity both in vitro and in vivo.

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Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Celecoxib	Prostaglandin G/H synthase 2	IC 50 (nM)	40	N/A	N/A	Details