Quantitative structure-activity relationship study of N-(3-oxo-3, 4-dihydro-2H-benzo [1, 4] thiazine-6-carbonyl) guanidines as potent Na/H exchange inhibitors.

T Yamamoto, M Hori, I Watanabe, K Harada…

Index: Yamamoto, Takeshi; Hori, Manabu; Watanabe, Ikuo; Harada, Kengo; Ikeda, Shoji; Ohtaka, Hiroshi Chemical and Pharmaceutical Bulletin, 2000 , vol. 48, # 6 p. 843 - 849

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Citation Number: 21

Abstract

We have previously reported that N-(4-isopropyl-2, 2-dimethyl-3-oxo-3, 4-dihydro-2H-benzo [1, 4] oxazine-6-carbonyl) guanidine (4b) methanesulfonate salt (KB-R9032) is a potent and highly water-soluble Na/H exchange inhibitor. In a series of studies on Na/H exchange inhibitors, we designed and synthesized N-(3-oxo-3, 4-dihydro-2H-benzo [1, 4] thiazine-6- carbonyl) guanidines (5) as more potent inhibitors with high water-solubility. The design ...