Literature DB >> 15026050

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 Singh1, Saibaba Vobbalareddy, Samala Shivaramakrishna, A Krishnamraju, Shaikh Abdul Rajjak, Seshagiri Rao Casturi, Vangoori Akhila, Yeleswarapu Koteswar Rao.   

Abstract

The effect of methanesulfonamide (MeSO(2)NH) 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.

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Year:  2004        PMID: 15026050     DOI: 10.1016/j.bmcl.2004.01.053

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  2 in total

1.  Selective COX-2 Inhibitors: A Review of Their Structure-Activity Relationships.

Authors:  Afshin Zarghi; Sara Arfaei
Journal:  Iran J Pharm Res       Date:  2011       Impact factor: 1.696

2.  Design, synthesis, biological assessment and in silico ADME prediction of new 2-(4-(methylsulfonyl) phenyl) benzimidazoles as selective cyclooxygenase-2 inhibitors.

Authors:  Mohamed A S Badawy; Eman K A Abdelall; El-Shaymaa El-Nahass; Khaled R A Abdellatif; Hamdy M Abdel-Rahman
Journal:  RSC Adv       Date:  2021-08-17       Impact factor: 4.036

  2 in total

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