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Synthesis and evaluation of a novel series of pseudo-cinnamic derivatives as antituberculosis agents. 2009
Georges Koumba Yoya, and
Florence Bedos-Belval, and
Patricia Constant, and
Hubert Duran, and
Mamadou Daffé, and
Michel Baltas
Université de Toulouse, UPS, LSPCMIB (Laboratoire de Synthèse et Physico-Chimie de Molécules d'Intérêt Biologique), 118, Route de Narbonne, F-31062 Toulouse Cedex 9, France.
In an effort to develop potent new antituberculous drugs effective against Mycobacterium tuberculosis, we have prepared series of cinnamic derivatives (thioesters and amides) with 4-hydroxy and 4-alkoxy groups and investigated the in vitro activities of these compounds. Among them some displayed a good in vitro antibacterial activity, such as (E)-N-(2-acetamidoethyl)-3-{4-[(E)-3,7-dimethylocta-2,6-dienyloxy]phenyl}acrylamide 4b that showed a minimum inhibitory concentration of 0.1microg/mL (0.26microM) against M. tuberculosis H37Rv.
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