Structural modifications of benzimidazoles via multi-step synthesis and their impact on sirtuin-inhibitory activity

Yeong Keng Yoon, Tan Soo Choon

Research output: Contribution to journalArticleResearchpeer-review

10 Citations (Scopus)

Abstract

Benzimidazole derivatives have been shown to possess sirtuin-inhibitory activity. In the continuous search for potent sirtuin inhibitors, systematic changes on the terminal benzene ring were performed on previously identified benzimidazole-based sirtuin inhibitors, to further investigate their structure-activity relationships. It was demonstrated that the sirtuin activities of these novel compounds followed the trend where meta-substituted compounds possessed markedly weaker potency than ortho- and para-substituted compounds, with the exception of halogenated substituents. Molecular docking studies were carried out to rationalize these observations. Apart from this, the methods used to synthesize the interesting compounds are also discussed.

Original languageEnglish
Pages (from-to)1-8
Number of pages8
JournalArchiv der Pharmazie
Volume349
Issue number1
DOIs
Publication statusPublished - Jan 2016
Externally publishedYes

Keywords

  • Benzimidazole
  • Molecular docking
  • SAR
  • Sirtuin

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