Synthesis and evaluation of a novel series of pseudo-cinnamic derivatives as antituberculosis agents.
Yoya GK, Bedos-Belval F, Constant P, Duran H, Daffé M, Baltas M.
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.