6466-95-1Relevant academic research and scientific papers
2-Hydroxy-substituted cinnamic acids and acetanilides are selective growth inhibitors of Mycobacterium tuberculosis
Guzman, Juan D.,Mortazavi, Parisa N.,Munshi, Tulika,Evangelopoulos, Dimitrios,McHugh, Timothy D.,Gibbons, Simon,Malkinson, John,Bhakta, Sanjib
, p. 47 - 50 (2014/01/06)
Selective chemical hits are required for feeding the initial discovery phase of the anti-tuberculosis therapeutics pipeline. These chemical entities should ideally target novel mechanisms of action in order to tackle drug resistance in Mycobacterium tuberculosis. In this work, hydroxycinnamic acid and acetamidophenol skeleta were employed for assessing the effects of constitutional isomerism on in vitro anti-TB activity. The whole cell evaluation of minimum inhibitory concentration values of different substituted cinnamic acids and acetamidophenols showed that the free ortho hydroxyl group conferred both potency and selectivity. Both 2-coumaric acid and 2-acetamidophenol showed minimum inhibitory concentration below 150 μM against M. tuberculosis H 37Rv and selectivity index higher than 30.
Synthesis and evaluation of a novel series of pseudo-cinnamic derivatives as antituberculosis agents
Yoya, Georges Koumba,Bedos-Belval, Florence,Constant, Patricia,Duran, Hubert,Daffe, Mamadou,Baltas, Michel
body text, p. 341 - 343 (2011/02/26)
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.
