1.
Bioorg Chem
; 51: 48-53, 2013 Dec.
Article
in English
| MEDLINE
| ID: mdl-24012092
ABSTRACT
A series of novel alkynyl substituted 3,4-dihydropyrimidin-2(1H)-one (DHPM) derivatives were designed, synthesized and evaluated in vitro as potential inhibitors of chorismate mutase (CM). All these compounds were prepared via a multi-component reaction (MCR) involving sequential I2-mediated Biginelli reaction followed by Cu-free Sonogashira coupling. Some of them showed promising inhibitory activities when tested at 30µM. One compound showed dose dependent inhibition of CM with IC50 value of 14.76±0.54µM indicating o-alkynylphenyl substituted DHPM as a new scaffold for the discovery of promising inhibitors of CM.