Synthesis and bioactivities of 2-azetidinone derivatives as cholesterol absorption inhibitors.
Twenty-four 2-azetidinone derivatives have been designed and synthesized as cholesterol absorption inhibitors. All new compounds were evaluated for their activity to inhibit cholesterol absorption in hamsters, and most of them showed considerable effects in lowering the levels of total cholesterol in the serum, especially compound 2d, 4a, 4f, 4i and 4j.
School of Pharmaceutical Sciences, Nanjing University of Technology, NO.5 Xinmofan Road, Nanjing 210009, China.
Yubin
Y
Wang
Hai
H
Qian
Jinpei
J
Zhou
Huibin
H
Zhang
Jianfeng
J
Ji
Wenlong
W
Huang
D000042:Absorption / Q000187:drug effects; D000818:Animals; D001384:Azetidines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D002784:Cholesterol / Q000008:administration & dosage / Q000097:blood / Q000378:metabolism*; D006224:Cricetinae; D015394:Molecular Structure; D013329:Structure-Activity Relationship
C116379:2-azetidinone; D001384:Azetidines; D002784:Cholesterol