5081-19-6Relevant academic research and scientific papers
Design, synthesis and inhibitory activity against human dihydroorotate dehydrogenase (hDHODH) of 1,3-benzoazole derivatives bearing amide units
Li, Jiling,Wu, Dang,Xu, Xiaoyong,Huang, Jin,Shao, Xusheng,Li, Zhong
supporting information, p. 3064 - 3066 (2016/06/13)
A series of 1,3-benzoazole derivatives possessing amide moieties were designed, synthesized and evaluated as inhibitors against human dihydroorotate dehydrogenase (hDHODH). Compounds A11, A14 and A26 exhibited good to excellent activities against hDHODH at the concentration of 10 μM. In particular, compound A14 displayed an IC50 value of 0.178 μM with 2-fold preference over A771726. 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.
