title: Synthesis and anti-hypercholesterolemic evaluations of calcium salts of 4-substituted quinoline-based mevalonic acid.
abstract: A series of calcium (3R,5S,6E)-7-[4,6,7,8-substituted-quinoline-3-yl]-3,5-dihydroxy-hept-6-enoates was synthesized from the lactones, and the anti-hypercholesterolemic evaluation in quails was presented in this report. It was found that most of the compounds significantly decreased levels of total cholesterol and low-density lipoprotein. 2e showed better hypolipidemic effect than atorvastatin, and 2d and 2j exhibited comparable efficacy to atorvastatin. These three compounds were selected as the hypocholesterolemic candidates for further evaluation.
authors.affiliation: State Key Lab of New Drug & Pharmaceutical Process, Shanghai Key Lab of Anti-Infectives, Shanghai Institute of Pharmaceutical Industry, State Institute of Pharmaceutical Industry, Shanghai 200437, China.
authors.forename: Qun
authors.initials: Q
authors.lastname: Hao
authors.forename: Zhengyan
authors.initials: Z
authors.lastname: Cai
authors.forename: Jing
authors.initials: J
authors.lastname: Pan
authors.forename: Yongjia
authors.initials: Y
authors.lastname: Li
authors.forename: Yuye
authors.initials: Y
authors.lastname: Xia
authors.forename: Yang
authors.initials: Y
authors.lastname: Min
authors.forename: Yuchen
authors.initials: Y
authors.lastname: Sheng
authors.forename: Weicheng
authors.initials: W
authors.lastname: Zhou
mesh_terms: D000818:Animals; D000924:Anticholesteremic Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000627:therapeutic use*; D002118:Calcium / Q000737:chemistry* / Q000627:therapeutic use*; D002784:Cholesterol / Q000378:metabolism; D006937:Hypercholesterolemia / Q000188:drug therapy*; D008077:Lipoproteins, LDL / Q000378:metabolism; D008297:Male; D008798:Mevalonic Acid / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D011784:Quail; D011804:Quinolines / Q000138:chemical synthesis / Q000737:chemistry / Q000627:therapeutic use; D012492:Salts / Q000138:chemical synthesis / Q000737:chemistry / Q000627:therapeutic use
chemical_list: D000924:Anticholesteremic Agents; D008077:Lipoproteins, LDL; D011804:Quinolines; D012492:Salts; D002784:Cholesterol; C037219:quinoline; D008798:Mevalonic Acid; D002118:Calcium