Synthesis and Antitubercular Activity of New L-serinyl Hydrazone Derivatives

Author(s): Alessandra Campbell Pinheiro, Carlos Roland Kaiser, Thais Cristina Mendonca Nogueira, Samir Aquino Carvalho, Edson Ferreira da Silva, Larisse de Oliveira Feitosa, Maria das Gracas Muller de Oliveira Henriques, Andre Luis Peixoto Candea, Maria Cristina Silva Lourenco, Marcus Vinicius Nora de Souza.

Journal Name: Medicinal Chemistry

Volume 7 , Issue 6 , 2011

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Abstract:

A series of 32 L-serinyl hydrazone derivatives have been synthesized and evaluated for their in vitro antibacterial activity against Mycobacterium tuberculosis H37Rv, being also evaluated their cell viabilities in non infected and infected macrophages with Mycobacterium bovis Bacillus Calmette-Guerin (BCG). The compounds 8c, 8e, 8h and 8i, were non-cytotoxic and exhibited an important minimum inhibitory concentration (MIC) activity between 25 and 100μg/mL, which can be compared with that of the tuberculostatic drug D-cicloserine (5-20μg/mL).

Keywords: BCG, D-cycloserine, hydrazone, L-cycloserine, L-serine, Mycobacterium, tuberculosis, L-serinyl hydrazone, tuberculostatic drug D-cicloserine, isoniazid and rifampin

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Article Details

VOLUME: 7
ISSUE: 6
Year: 2011
Page: [611 - 623]
Pages: 13
DOI: 10.2174/157340611797928325
Price: $58

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