E. Sartori, F. Camy, J. Teulon
1993
Citations
0
Influential Citations
6
Citations
Quality indicators
Journal
European Journal of Medicinal Chemistry
Abstract
Abstract 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 A 2 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-[(4-chloro-benzenesulfonylaminoethyl)thio] 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 .