title: Novel potassium channel openers. Part 4: transformation of the 1,4-benzoxazine skeleton into 1,4-benzothiazine, 1,2,3,4-tetrahydroquinoline, 1,2,3,4-tetrahydroquinoxaline, indoline, and 1,5-benzoxazepine.
abstract: As part of a search for a new potassium channel opener, the 1,4-benzoxazine skeleton derived from the benzopyran skeleton of cromakalim, was transformed into other fused rings such as 1,4-benzothiazine, 1,2,3,4-tetrahydroquinoline, 1,2,3,4-tetrahydroquinoxaline, indoline, and 1,5-benzoxazepine. The 1,4-benzothiazine derivative displayed approximately 20 times more potent vasorelaxant activity than cromakalim.
authors.affiliation: Institute for Drug Discovery Research, Yarmanouchi Pharmaceutical Co., Ltd., Tsukuba, Ibaraki, Japan. matsumoy@yamanouchi.co.jp
authors.forename: Y
authors.initials: Y
authors.lastname: Matsumoto
authors.forename: R
authors.initials: R
authors.lastname: Tsuzuki
authors.forename: A
authors.initials: A
authors.lastname: Matsuhisa
authors.forename: Y
authors.initials: Y
authors.lastname: Yamagiwa
authors.forename: I
authors.initials: I
authors.lastname: Yanagisawa
authors.forename: T
authors.initials: T
authors.lastname: Shibanuma
authors.forename: H
authors.initials: H
authors.lastname: Nohira
mesh_terms: D000818:Animals; D004285:Dogs; D005260:Female; D066298:In Vitro Techniques; D008297:Male; D015221:Potassium Channels / Q000187:drug effects*
chemical_list: D015221:Potassium Channels