title: Total synthesis and antihypertensive activity of (+/-)7,8-dihydroxy-3-methyl-isochromanone-4.
abstract: This letter describes the total synthesis, preliminary biological evaluation and mechanism studies of a novel and structurally unique isochromanone, (+/-)7,8-dihydroxy-3-methyl-isochromanone-4 (1), a nature product contained in banana (Musa sapientum L.) peel. The bioassay showed that compound 1 displays potent antihypertensive activity in renal hypertensive rats and further mechanism studies revealed that it is an ACE inhibitor.
authors.affiliation: Department of Medicinal Chemistry, China Pharmaceutical University, Tongjia Xiang 24, Nanjing, Jiangsu 210009, China.
authors.forename: Jie
authors.initials: J
authors.lastname: Liu
authors.forename: Hao
authors.initials: H
authors.lastname: Ren
authors.forename: Jinyi
authors.initials: J
authors.lastname: Xu
authors.forename: Renren
authors.initials: R
authors.lastname: Bai
authors.forename: Qi
authors.initials: Q
authors.lastname: Yan
authors.forename: Wenlong
authors.initials: W
authors.lastname: Huang
authors.forename: Xiaoming
authors.initials: X
authors.lastname: Wu
authors.forename: Jihua
authors.initials: J
authors.lastname: Fu
authors.forename: Qiujuan
authors.initials: Q
authors.lastname: Wang
authors.forename: Qian
authors.initials: Q
authors.lastname: Wu
authors.forename: Rong
authors.initials: R
authors.lastname: Fu
mesh_terms: D000806:Angiotensin-Converting Enzyme Inhibitors / Q000737:chemistry* / Q000494:pharmacology; D000818:Animals; D000959:Antihypertensive Agents / Q000737:chemistry* / Q000494:pharmacology; D002626:Chemistry, Pharmaceutical / Q000379:methods*; D002867:Chromones / Q000737:chemistry* / Q000494:pharmacology; D015195:Drug Design; D006977:Hypertension, Renal / Q000188:drug therapy* / Q000378:metabolism; D008099:Liver / Q000187:drug effects; D008956:Models, Chemical; D015394:Molecular Structure; D028521:Musa / Q000378:metabolism; D010936:Plant Extracts / Q000494:pharmacology; D051381:Rats; D013329:Structure-Activity Relationship
chemical_list: C542962:7,8-dihydroxy-3-methyl-isochromanone-4; D000806:Angiotensin-Converting Enzyme Inhibitors; D000959:Antihypertensive Agents; D002867:Chromones; D010936:Plant Extracts