title: Synthesis and evaluation of a novel series of pseudo-cinnamic derivatives as antituberculosis agents.
abstract: 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.
authors.affiliation: 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.
authors.forename: Georges Koumba
authors.initials: GK
authors.lastname: Yoya
authors.forename: Florence
authors.initials: F
authors.lastname: Bedos-Belval
authors.forename: Patricia
authors.initials: P
authors.lastname: Constant
authors.forename: Hubert
authors.initials: H
authors.lastname: Duran
authors.forename: Mamadou
authors.initials: M
authors.lastname: Daffé
authors.forename: Michel
authors.initials: M
authors.lastname: Baltas
mesh_terms: 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
chemical_list: D000995:Antitubercular Agents; D002934:Cinnamates; C029010:cinnamic acid