Methanesulfonamide group at position-4 of the C-5-phenyl ring of 1,5-diarylpyrazole affords a potent class of cyclooxygenase-2 (COX-2) inhibitors

Sunil Kumar Singh; Saibaba Vobbalareddy; Samala Shivaramakrishna; A. Krishnamraju; Shaikh Abdul Rajjak; Seshagiri Rao Casturi; Vangoori Akhila; Yeleswarapu Koteswar Rao

doi:10.1016/j.bmcl.2004.01.053

Back

Methanesulfonamide group at position-4 of the C-5-phenyl ring of 1,5-diarylpyrazole affords a potent class of cyclooxygenase-2 (COX-2) inhibitors

Journal article

Peer reviewed

Methanesulfonamide group at position-4 of the C-5-phenyl ring of 1,5-diarylpyrazole affords a potent class of cyclooxygenase-2 (COX-2) inhibitors

Sunil Kumar Singh, Saibaba Vobbalareddy, Samala Shivaramakrishna, A. Krishnamraju, Shaikh Abdul Rajjak, Seshagiri Rao Casturi, Vangoori Akhila and Yeleswarapu Koteswar Rao

Bioorganic & medicinal chemistry letters, Vol.14(7), pp.1683-1688

05/04/2004

DOI: https://doi.org/10.1016/j.bmcl.2004.01.053

PMID: 15026050

Abstract

1,5-diarylpyrazoles

Cyclooxygenase-2 inhibitors

Methanesulfonamide

The effect of methanesulfonamide (MeSO 2NH) group on COX-2 inhibitory activity of 1,5-diarylpyrazole is described. While this group being at position-4 of the N 1-phenyl ring was found to be ineffective, its installation at position-4 of the C-5 phenyl ring offered several potent and selective inhibitors of COX-2 with IC 50 as low as 30 nM. The effect of methanesulfonamide (MeSO 2NH) group on COX-2 inhibitory activity of 1,5-diarylpyrazole is described.

Metrics

1 Record Views

See more details

Details

Title: Methanesulfonamide group at position-4 of the C-5-phenyl ring of 1,5-diarylpyrazole affords a potent class of cyclooxygenase-2 (COX-2) inhibitors
Creators - without role: Sunil Kumar Singh - Dr. Reddy's Laboratories
Saibaba Vobbalareddy - Dr. Reddy's Laboratories
Samala Shivaramakrishna - Dr. Reddy's Laboratories
A. Krishnamraju - Dr. Reddy's Laboratories
Shaikh Abdul Rajjak - Dr. Reddy's Laboratories
Seshagiri Rao Casturi - Dr. Reddy's Laboratories
Vangoori Akhila - Discovery Biology, Discovery Research-Dr. Reddy's Laboratories Ltd, Bollaram Road, Miyapur, Hyderabad 500 049, India
Yeleswarapu Koteswar Rao - Discovery Chemistry, Discovery Research-Dr. Reddy's Laboratories Ltd, Bollaram Road, Miyapur, Hyderabad 500 049, India
Publication Details: Bioorganic & medicinal chemistry letters, Vol.14(7), pp.1683-1688
Publisher: Elsevier Ltd
Identifiers: 9945302608331
Academic Unit: King Abdullah University of Science & Technology
Language: English
Resource Type: Journal article