Synthesis and evaluation of a novel series of pseudo-cinnamic derivatives as antituberculosis agents.
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.
Yoya
Georges Koumba
GK
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.
Bedos-Belval
Florence
F
Constant
Patricia
P
Duran
Hubert
H
Daffé
Mamadou
M
Baltas
Michel
M
D000995:Antitubercular Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D002934:Cinnamates / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D008826:Microbial Sensitivity Tests; D009169:Mycobacterium tuberculosis / Q000187:drug effects
D000995:Antitubercular Agents; D002934:Cinnamates; C029010:cinnamic acid