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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.

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.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Singh SK,Vobbalareddy S,Shivaramakrishna S,Krishnamraju A,Rajjak SA,Casturi SR,Akhila V,Rao YK

doi

10.1016/j.bmcl.2004.01.053

subject

Has Abstract

pub_date

2004-04-05 00:00:00

pages

1683-8

issue

7

eissn

0960-894X

issn

1464-3405

pii

S0960894X04001337

journal_volume

14

pub_type

杂志文章

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