New N-aryl-4-(methysulfony)aminobenzenesulfonamid es as selective COX-2 inhibitors

Moallem, S. A. and Hadizadeh, F. and Yavar, I. (2011) New N-aryl-4-(methysulfony)aminobenzenesulfonamid es as selective COX-2 inhibitors. Journal of Biological Sciences, 11 (8). pp. 496-499.

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A group of N-aryl- 4-(methylsulfonyl)aminobenzenesulfonamides, possessing a (methylsulfonyl) amino pharmacophore at the para-position of the one phenyl ring, in conjunction with another substituted phenyl ring (4-F, 4-H, 4-Me, 4-OMe) were evaluated as selective cyclooxygenase-2 (COX-2) inhibitors. In vitro COX-2 isozyme inhibition structure-activity studies identified 6e with 4-OMe substituent as a potent COX-2 inhibitor (IC 50 = 1.59 juM) with a high COX-2 selectivity index (SI = 51.7) comparable to the reference drug celecoxib (COX-2 IC 50 = 9.59 juM; COX-2 SI = 25.62). The structure-activity data acquired indicate that the sulfonamido moiety constitutes a suitable scaffold to design new acyclic N-aryl- 4-(methysulfonyl)aminobenzenesulfonamides derivatives with selective COX-2 inhibitoiy activity. © 2011 Asian Network for Scientific Information.

Item Type: Article
Additional Information: Cited By :2 Export Date: 16 February 2020 Correspondence Address: Hadizadeh, F.; Biotechnology Research Center, Mashhad University of Medical Sciences, Mashhad, Iran
Uncontrolled Keywords: Benzenesulfonamides COX-2 inhibitors 1,3 diarylthiourea celecoxib cyclooxygenase 2 inhibitor etorcoxib n aryl 4 (methysulfony)aminobenzenesulfonamide derivative rofecoxib unclassified drug valdecoxib article in vitro study molecular model structure activity relation
Subjects: QV pharmacology
Divisions: Mashhad University of Medical Sciences
Depositing User: mr lib7 lib7
Date Deposited: 05 May 2020 04:02
Last Modified: 05 May 2020 04:02

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