Abstract
Abstract A number of phenylsulfonamido derivatives have been synthesized and tested for their ability to inhibit: a) thromboxane A 2 /prostaglandin H 2 ( TXA 2 PGH 2 ) mimetic (U46619)- induced guinea pig platelet aggregation; b) aortic ring contraction; and c) binding of a radioiodinated TXA 2 PGH 2 mimetic (I-BOP) to platelets. In platelet, K d values ranged from 9 nM to > 50 μM. p K b values in aortic rings ranged from 7.63 to 3.66 and in platelets from 7.7 to K d and p K b values found in the 3 systems. Antagonist activity at the TXA 2 PGH 2 receptor was sensitive to both the substitution pattern of the 2 aromatic rings and the presence of heteroatoms. For 2 of the derivatives ( 4 and 11 ) molecular mechanics calculations were performed which indicated subtle structural differences that may account for the > 300-fold difference in potency observed for these analogs at the platelet TXA 2 PGH 2 receptor.
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