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    Antimicrob Agents Chemother. 2007 Feb;51(2):752-4. Epub 2006 Nov 13.

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

    Zimhony O, Vilchèze C, Arai M, Welch JT, Jacobs WR Jr.

    Source

    Infectious Diseases Division, Kaplan Medical Center, The Hebrew University and Hadassah Jerusalem, P.O. Box 1, Rehovot 76100, Israel. oren_z@clalit.org.il

    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.

    PMID:
    17101678
    [PubMed - indexed for MEDLINE]
    PMCID:
    PMC1797748
    Free PMC Article

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