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
Medicinal Chemistry
Title: Synthesis and Antitubercular Activity of New L-serinyl Hydrazone Derivatives
Volume: 7 Issue: 6
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 and Marcus Vinicius Nora de Souza
Affiliation:
Keywords: BCG, D-cycloserine, hydrazone, L-cycloserine, L-serine, Mycobacterium, tuberculosis, L-serinyl hydrazone, tuberculostatic drug D-cicloserine, isoniazid and rifampin
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).
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Campbell Pinheiro Alessandra, Roland Kaiser Carlos, Cristina Mendonca Nogueira Thais, Aquino Carvalho Samir, Ferreira da Silva Edson, de Oliveira Feitosa Larisse, das Gracas Muller de Oliveira Henriques Maria, Luis Peixoto Candea Andre, Cristina Silva Lourenco Maria and Vinicius Nora de Souza Marcus, Synthesis and Antitubercular Activity of New L-serinyl Hydrazone Derivatives, Medicinal Chemistry 2011; 7 (6) . https://dx.doi.org/10.2174/157340611797928325
DOI https://dx.doi.org/10.2174/157340611797928325 |
Print ISSN 1573-4064 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-6638 |
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