1025895-59-3Relevant academic research and scientific papers
Synthesis and evaluation of novel sulfonamide derivatives as thromboxane A2 receptor antagonists I
Sato, M.,Kawashima, Y.,Goto, J.,Yamane, Y.,Chiba, Y.,et al.
, p. 185 - 190 (2007/10/02)
A series of 4-phenoxyacetic acids and related compounds were synthesized.The compounds were tested for their thromboxane A2 (TXA2) receptor antagonizing effects on (15S)-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-phenyl>propionic acids 26a-e,g showed potent TXA2 receptor antagonist activity.The most potent compound, 3-phenyl>propionic acid 26c was more than 10-fold more potent in TXA2 receptor antagonizing activity (IC50 = 1.1*106 M) than sulotroban (BM-13177) on rabbit platelets.Compound 26c was also more than 10-fold more potent in TXA2-inhibitory activity than sulotroban on rat aorta smooth muscle (pA2 7.7) thromboxane A2 / TXA2 / receptor antagonist / sulfonamide derivative / sulotroban
