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