Thromboxane A2 receptor antagonists. Synthesis and activities of phenylsulfonamido derivatives

…, F Mohamadi, GP Dube, WL Kurtz, KA Brune…

Index: Mais, DE; Mohamadi, F; Dube, GP; Kurtz, WL; Brune, KA; et al. European Journal of Medicinal Chemistry, 1991 , vol. 26, # 8 p. 821 - 827

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Citation Number: 11

Abstract

Abstract A number of phenylsulfonamido derivatives have been synthesized and tested for their ability to inhibit: a) thromboxane A 2/prostaglandin H 2 (TXA2PGH2) mimetic (U46619)- induced guinea pig platelet aggregation; b) aortic ring contraction; and c) binding of a radioiodinated TXA2PGH2 mimetic (I-BOP) to platelets. In platelet, K d values ranged from 9 nM to> 50 μM. pK b values in aortic rings ranged from 7.63 to 3.66 and in platelets from ...