Design, synthesis and inhibitory activity against human dihydroorotate dehydrogenase (hDHODH) of 1, 3-benzoazole derivatives bearing amide units. Issue 13 (1st July 2016)

• Record Type: Journal Article
• Authors: Li, Jiling; Wu, Dang; Xu, Xiaoyong; huang, Jin; Shao, Xusheng; Li, Zhong
• Is Part Of: Bioorganic & medicinal chemistry letters. Volume 26:Issue 13(2016)
• Page Start: 3064
• Page End: 3066
• Publication Date: 2016-07-01
• Subjects: 1, 3-Benzoazole -- hDHODH -- Activity -- Amide -- Scaffold hopping; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; 572
• DOI: 10.1016/j.bmcl.2016.05.016
• Languages: English
• ISSNs: 0960-894X

Abstract

Graphical abstract: Abstract: A series of 1, 3-benzoazole derivatives possessing amide moieties were designed, synthesized and evaluated as inhibitors against human dihydroorotate dehydrogenase ( h DHODH). CompoundsA11, A14 andA26 exhibited good to excellent activities against h DHODH at the concentration of 10 μM. In particular, compoundA14 displayed an IC50 value of 0.178 μM with 2-fold preference overA771726 . The result implied that a proper degree of steric size and electron density of the C-6 amide moiety was necessary to retain the inhibitory activity of the synthesized compounds.