Synthesis of a series of novel 2,4,5-trisubstituted selenazole compounds as potential PLTP inhibitors.
Based on a homology-modeled structure of PLTP and characteristic structural features of reported cholesteryl ester transfer protein (CETP) inhibitors, we designed and synthesized a novel series of 2,4,5-trisubstituted selenazole compounds. Biological evaluation reveals that compounds 12 and 17 exhibit favorable PLTP activity, and their IC(50)s are 8 microM and 10 microM, respectively.
Ling
Cui
C
Laboratory of Computer-Aided Drug Design & Discovery, Beijing Institute of Pharmacology and Toxicology, Beijing, PR China.
Zheng
Zhibing
Z
Jiang
Xian Cheng
XC
Zhong
Wu
W
Li
Song
S
D001393:Azoles / Q000737:chemistry*; D004353:Drug Evaluation, Preclinical; D020128:Inhibitory Concentration 50; D049294:Phospholipid Transfer Proteins / Q000037:antagonists & inhibitors*; D018036:Selenium Compounds / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*
D001393:Azoles; D049294:Phospholipid Transfer Proteins; D018036:Selenium Compounds