Pyrazinoic acid and its n-propyl ester inhibit fatty acid synthase type I in replicating tubercle bacilli

Oren Zimhony, Catherine Vilchèze, Masayoshi Arai, John T. Welch, William R. Jacobs

Research output: Contribution to journalArticle

77 Scopus citations

Abstract

The activity of different analogs of pyrazinamide on Mycobacterium tuberculosis fatty acid synthase type I (FASI) in replicating bacilli was studied. Palmitic acid biosynthesis was diminished by 96% in bacilli treated with n-propyl pyrazinoate, 94% in bacilli treated with 5-chloro-pyrazinamide, and 97% in bacilli treated with pyrazinoic acid, the pharmacologically active agent of pyrazinamide. We conclude that the minimal structure of pyrazine ring with an acyl group is sufficient for FASI inhibition and antimycobacterial activity.

Original languageEnglish (US)
Pages (from-to)752-754
Number of pages3
JournalAntimicrobial agents and chemotherapy
Volume51
Issue number2
DOIs
StatePublished - Feb 2007

ASJC Scopus subject areas

  • Pharmacology
  • Pharmacology (medical)
  • Infectious Diseases

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