5-Arylaminouracil Derivatives: New Inhibitors of Mycobacterium tuberculosis
Elena Matyugina, Mikhail Novikov, Denis Babkov, Alexander Ozerov, Larisa Chernousova, Sofia Andreevskaya, Tatiana Smirnova, Inna Karpenko, Alexander Chizhov, Pravin Murthu, Stefan Lutz, Sergei Kochetkov, Katherine L. Seley-Radtke and Anastasia L. Khandazhinskaya
Article first published online: 14 JUL 2015 | DOI: 10.1111/cbdd.12603
Three series of 5-arylaminouracil derivatives were synthesized and screened for potential antimicrobial activity. Most of compounds had a negative effect on the growth of the M. tuberculosis H37Rv strain, with 100% inhibition observed at concentrations between 5 and 40 μg/mL. Of those, 1-(4′-hydroxy-2′-cyclopenten-1′-yl)-3-(4‴-hydroxy-2‴-cyclopenten-1‴-yl)-5-(4″-butyloxyphenylamino)uracil proved to be the most active among tested compounds against the M. tuberculosis multidrug-resistant strain MS-115 (MIC90 5 μg/mL).