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

doi:10.1128/AAC.01369-06

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

Chemistry

University at Albany

Hebrew University of Jerusalem
Albert Einstein College of Medicine

Research output: Contribution to journal › Article › peer-review

93 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 language	English
Pages (from-to)	752-754
Number of pages	3
Journal	Antimicrobial Agents and Chemotherapy
Volume	51
Issue number	2
DOIs	https://doi.org/10.1128/AAC.01369-06
State	Published - Feb 2007

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

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.",

author = "Oren Zimhony and Catherine Vilch{\`e}ze and Masayoshi Arai and Welch, \{John T.\} and Jacobs, \{William R.\}",

year = "2007",

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T1 - Pyrazinoic acid and its n-propyl ester inhibit fatty acid synthase type I in replicating tubercle bacilli

AU - Zimhony, Oren

AU - Vilchèze, Catherine

AU - Arai, Masayoshi

AU - Welch, John T.

AU - Jacobs, William R.

PY - 2007/2

Y1 - 2007/2

N2 - 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.

AB - 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.

UR - https://www.scopus.com/pages/publications/33846605483

U2 - 10.1128/AAC.01369-06

DO - 10.1128/AAC.01369-06

M3 - Article

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SN - 0066-4804

VL - 51

SP - 752

EP - 754

JO - Antimicrobial Agents and Chemotherapy

JF - Antimicrobial Agents and Chemotherapy

IS - 2

ER -

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

Abstract

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