749206-08-4Relevant academic research and scientific papers
Synthesis and activities of new arylsulfonamido thromboxane A2 receptor antagonists
Sartori, E.,Camy, F.,Teulon, J. M.,Caussade, F.,Virone-Oddos, A.,Cloarec, A.
, p. 625 - 632 (2007/10/02)
New benzoic, benzeneacetic and thiazole-4-acetic acids bearing an arylsulfonamido alkyl or alkylhetero side chain were synthesized and tested in vitro for affinity for human platelet thromboxane A2 receptors and inhibition of U46619-induced rat aortic ring contraction.Influence of substitution patterns, chain length and presence of heteroatoms were studied and compounds within a 30 nmol range for inhibition of U46619-induced contractions were found.One of the most potent, 2-thiazole-4-acetic acid (VII-4) was orally active (1 mg/kg), as evidenced by the inhibition of U46619-induced platelet aggregation in guinea pigs, ex vivo. thromboxane A2 / receptor antagonist / platelet aggregation / arylsulfonamido derivative
