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
Letters in Drug Design & Discovery
Title: Synthesis and Cyclooxygenase-2 (COX-2) Inhibiting Properties of 1,5- Diarylpyrazoles Possessing N-Substitution on the Sulfonamide (-SO2NH2) Moiety †
Volume: 2 Issue: 4
Author(s): Manojit Pal, Venugopal Rao Veeramaneni, Sanjeev Kumar, Akhila Vangoori, Ramesh Mullangi, Parimal Misra, Shaikh Abdul Rajjak, Vidya B. Lohray, Seshagiri Rao Casturi and Koteswar Rao Yeleswarapu
Affiliation:
Keywords: diarylpyrazoles, cox, &, cox inhibition, structure activity relationship (sar) study
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.
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Pal Manojit, Veeramaneni Rao Venugopal, Kumar Sanjeev, Vangoori Akhila, Mullangi Ramesh, Misra Parimal, Rajjak Abdul Shaikh, Lohray B. Vidya, Casturi Rao Seshagiri and Yeleswarapu Rao Koteswar, Synthesis and Cyclooxygenase-2 (COX-2) Inhibiting Properties of 1,5- Diarylpyrazoles Possessing N-Substitution on the Sulfonamide (-SO2NH2) Moiety †, Letters in Drug Design & Discovery 2005; 2 (4) . https://dx.doi.org/10.2174/1570180054038459
DOI https://dx.doi.org/10.2174/1570180054038459 |
Print ISSN 1570-1808 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-628X |
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