Synthesis and evaluation of a novel series of pseudo-cinnamic derivatives as antituberculosis agents

Georges Koumba Yoya (1) , Florence Bedos-Belval (1) , Patricia Constant (2) , Hubert Duran (1) , Mamadou Daffé (2) , Michel Baltas (1)

1 SPCMIB - Synthèse et Physico-Chimie de Molécules d'Intérêt Biologique
2 IPBS - Institut de pharmacologie et de biologie structurale

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 0.1 μg/mL (0.26 μM) against M. tuberculosis H37Rv.

Mots clés: Cinnamic derivatives; Antituberculosis agents; Mycobacterium tuberculosis; TB MIC

Domaines: Sciences pharmaceutiques

Georges Koumba Yoya, Florence Bedos-Belval, Patricia Constant, Hubert Duran, Mamadou Daffé, et al.. Synthesis and evaluation of a novel series of pseudo-cinnamic derivatives as antituberculosis agents. Bioorganic and Medicinal Chemistry Letters, 2009, 19 (2), pp.341-343. ⟨10.1016/j.bmcl.2008.11.082⟩. ⟨hal-03102436⟩