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.
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.
Matsumoto
Y
Y
Institute for Drug Discovery Research, Yarmanouchi Pharmaceutical Co., Ltd., Tsukuba, Ibaraki, Japan. matsumoy@yamanouchi.co.jp
Tsuzuki
R
R
Matsuhisa
A
A
Yamagiwa
Y
Y
Yanagisawa
I
I
Shibanuma
T
T
Nohira
H
H
D000818:Animals; D004285:Dogs; D005260:Female; D066298:In Vitro Techniques; D008297:Male; D015221:Potassium Channels / Q000187:drug effects*
D015221:Potassium Channels