Study on N-(pyridin-4-Yl) Salicylamides as Antimycobacterial Agents

Author:

Xin Zhi Jun1,Jia Zhong2,He Dian3,Liang Jian Ping1,Tao Lei1,Li Xue Hu4,Lu Xi Hong4

Affiliation:

1. Institute of Modern Physics, Chinese Academy of Sciences

2. Lanzhou City China Medicine Hospital

3. Lanzhou University

4. Chinese Academy of Sciences

Abstract

A series of N-(pyridin-4-yl) salicylamides derivatives were prepared through acylation of the corresponding acetylsalicyloyl chlorides with substituted 4-amino-pyridines. These compounds were evaluated in vitro for antimycobacterial activities against Mycobacterium tuberculosis (TB) and Mycobacterium avium (A) by the minimum inhibitory concentrations (MIC) values. Eight of the compounds exhibited lower MIC against A than isoniazide (INH). Meanwhile, four of the compounds exhibited good anti-TB activity, when they were compared with INH. Antimycobacterial activities of N-(pyridin-4-yl) salicylamides were influenced by the balance between hydrophobicity and electron-withdrawing substituent effect on the phenyl and pyridine ring. These studies show that these compounds might serve as prospective wide-spectrum antimycobacterial substances.

Publisher

Trans Tech Publications, Ltd.

Subject

General Engineering

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5. J.A. Hoch and T.J. Silhavy: Two-component Signal Transduction, ASM Press Publications, Washington, D.C. (1995), p.305.

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