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Design of novel N-phenylnicotinamides as selective cyclooxygenase-1 inhibitors

Authors
Journal
Bioorganic & Medicinal Chemistry Letters
0960-894X
Publisher
Elsevier
Publication Date
Volume
21
Issue
1
Identifiers
DOI: 10.1016/j.bmcl.2010.11.062
Keywords
  • Cyclooxygenase-1
  • Inhibitor
  • N-Phenylnicotinamide
  • Structure–Activity Relationship
  • Molecular Docking
Disciplines
  • Biology
  • Design

Abstract

Graphical abstract A series of N-phenylnicotinamides (1–40) were designed and evaluated in vitro for their COX inhibitory activities. Most of the synthesized compounds were proved to be potent and selective inhibitors of COX-1. Compound 28 showed the most potent COX-1 inhibitory activity (COX-1 IC50=0.68±0.07μM) and good selectivity (COX-2 IC50>100μM). This compound may be useful as a lead compound for superior COX-1 inhibitors. On the basis of the biological results, structure–activity relationships for the COX-1-inhibitory activities of the synthesized N-phenylnicotinamides were discussed concisely.

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