Abstract
A series of 4-[2-(arylsulfonylamino)ethylthio]phenoxyacetic acids and related compounds were synthesized. The compounds were tested for their thromboxane A 2 (TXA 2) receptor antagonizing effects on (15 S)-15-hydroxy-11a,9a-(epoxymethano)prosta-5( Z),13( E)-dienoic acid (U-46619)-induced aggregation of rabbit platelet-rich plasma (PRP). Among the compounds synthesized, 3-{4-[2-(arylsulfonylamino)ethylthio]phenyl}propionic acids 26a-e,g showed potent TXA 2 receptor antagonist activity. The most potent compound, 3-{4-[2-(4-chlorophenylsulfonylamino)ethylthio]phenyl}propionic acid 26c was more than 10-fold more potent in TXA 2 receptor antagonizing activity (IC 50 = 1.1 × 10 −6 M) than sulotroban (BM-13177) on rabbit platelets. Compound 26c was also more than 10-fold more potent in TXA 2-inhibitory activity than sulotroban on rat aorta smooth muscle ( pA 2 7.7).
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