… 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, …

Y Matsumoto, R Tsuzuki, A Matsuhisa, T Yoden…

Index: Matsumoto, Yuzo; Tsuzuki, Ryuji; Matsuhisa, Akira; Yoden, Toru; Yamagiwa, Yoko; Yanagisawa, Isao; Shibanuma, Tadao; Nohira, Hiroyuki Bioorganic and Medicinal Chemistry, 2000 , vol. 8, # 2 p. 393 - 404

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Citation Number: 40

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.