Novel 5-substituted 1H-tetrazoles as cyclooxygenase-2 (COX-2) inhibitors.

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Al-Hourani BJ, Sharma SK, Suresh M, Wuest F

Novel 5-substituted 1H-tetrazoles as cyclooxygenase-2 (COX-2) inhibitors.

Bioorg Med Chem Lett. 2012 Mar 15;22(6):2235-8. doi: 10.1016/j.bmcl.2012.01.093. Epub 2012 Feb 2.

PubMed ID

22341941 [ View in PubMed

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Abstract

A series of novel 5-substituted 1H-tetrazoles as cyclooxygenase-2 (COX-2) inhibitors was prepared via treatment of various diaryl amides with tetrachlorosilane/sodium azide. All compounds were tested in cyclooxygenase (COX) assays in vitro to determine COX-1 and COX-2 inhibitory potency and selectivity. Tetrazoles contained a methylsulfonyl or sulfonamide group as COX-2 pharmacophore displayed only low inhibitory potency towards COX-2. Most potent compounds showed IC(50) values of 6 and 7 muM for COX-2. All compounds showed IC(50) values greater 100 muM for COX-1 inhibition.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Celecoxib	Prostaglandin G/H synthase 2	IC 50 (nM)	60	N/A	N/A	Details