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  • Title: Novel alkynyl substituted 3,4-dihydropyrimidin-2(1H)-one derivatives as potential inhibitors of chorismate mutase.
    Author: Mallikarjuna Rao V, Mahesh Kumar P, Rambabu D, Kapavarapu R, Shobha Rani S, Misra P, Pal M.
    Journal: Bioorg Chem; 2013 Dec; 51():48-53. PubMed ID: 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.
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