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ChemInform Abstract: Design, Synthesis and Quantitative Structure—Activity Relationship Study of N-(3-Oxo-3,4-dihydro-2H-benzo[1,4]oxazine-7-carbonyl)guanidine Derivatives as Potent Na/H Exchange Inhibitors.

✍ Scribed by T. YAMAMOTO; M. HORI; I. WATANABE; H. TSUTSUI; K. HARADA; S. IKEDA; J. MARUO; T. MORITA; H. OHTAKA

Publisher
John Wiley and Sons
Year
2010
Weight
42 KB
Volume
29
Category
Article
ISSN
0931-7597

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✦ Synopsis

Design, Synthesis and Quantitative Structure-Activity Relationship Study of 4]oxazine-7carbonyl)guanidine Derivatives as Potent Na/H Exchange Inhibitors.

-A series of racemic as well as optically active (benzoxazine-7carbonyl)guanidine derivatives (VIII) are designed and synthesized starting from 4-amino-3-hydroxybenzoate (I). Structure-activity studies reveal a parabolical relationship between chain length and inhibitory activity.

The optically active compounds are the most potent inhibitors of Na/H exchange.

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