Synthesis and Cyclooxygenase-2 (COX-2) Inhibiting Properties of 1,5- Diarylpyrazoles Possessing N-Substitution on the Sulfonamide (-SO2NH2) Moiety†

Authors: Pal, Manojit; Veeramaneni, Venugopal R.; Kumar, Sanjeev; Vangoori, Akhila; Mullangi, Ramesh; Misra, Parimal; Rajjak, Shaikh A.b.d.u.l.; Lohray, Vidya B.; Casturi, Seshagiri R.a.o.; Yeleswarapu, Koteswar R.a.o.

Source: Letters in Drug Design & Discovery, Volume 2, Number 4, June 2005 , pp. 329-340(12)

Publisher: Bentham Science Publishers

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Abstract:

A number of novel 1,5-diarylpyrazoles possessing N-substitution on the sulfonamide (-SO2NH2) moiety were synthesized and tested for COX-1/COX-2 inhibition in vitro. Many of these 1,1-dioxo-2,3- dihydrobenzo[d]isothiazolyl substituted 1,5-diarylpyrazoles, where the SO2NH2 group was a part of the fused ring, showed COX inhibitory activity. Few of them were identified as selective COX-2 inhibitors. Structure Activity Relationship study within the series are discussed.

Keywords: diarylpyrazoles; cox & cox inhibition; structure activity relationship (sar) study

Document Type: Review article

DOI: http://dx.doi.org/10.2174/1570180054038459

Affiliations: 1: Discovery Research, Dr. Reddy's Laboratories Ltd., Bollaram Road, Miyapur, Hyderabad 500049, India.

Publication date: 2005-06-01

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  • Letters in Drug Design & Discovery publishes original letters on all areas of rational drug design and discovery including medicinal chemistry, in-silico drug design, combinatorial chemistry, high-throughput screening, drug targets, and structure-activity relationships. The emphasis will be on publishing quality papers very rapidly. Letters will be processed rapidly by taking full advantage of Internet technology for both the submission and review of manuscripts. The journal is essential reading to all pharmaceutical scientists involved in research in drug design and discovery.

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