Archiv der Pharmazie

New NO??Donors with Antithrombotic and Vasodilating Activities, Part 16 3??Amino??1, 2, 4??oxadiazol??5??ones as Prodrugs for Hydroxyguanidines

K Rehse, S Bade

Index: Rehse, Klaus; Bade, Stephan Archiv der Pharmazie, 1996 , vol. 329, # 12 p. 535 - 540

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Citation Number: 5

Abstract

Abstract Nineteen 4-substituted 1, 2, 4-oxadiazol-5-ones (6a-s) were prepared as prodrugs for lipophilic hydroxyguanidines which should be metabolized in vivo to nitric oxide. This hypothesis was tested indirectly by measuring the antithrombotic properties of these compounds 2 h after oral administration to rats (60 mg/kg). In mesenteric arterioles seven compounds moderately (≥ 10%) inhibited the formation of thrombi by a laser beam. ...

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