773875-80-2Relevant articles and documents
Structural studies of pterin-based inhibitors of dihydropteroate synthase
Hevener, Kirk E.,Yun, Mi-Kyung,Qi, Jianjun,Kerr, Iain D.,Babaoglu, Kerim,Hurdle, Julian G.,Balakrishna, Kanya,White, Stephen W.,Lee, Richard E.
, p. 166 - 177 (2010)
Dihydropteroate synthase (DHPS) is a key enzyme in bacterial folate synthesis and the target of the sulfonamide class of antibacterials. Resistance and toxicities associated with sulfonamides have led to a decrease in their clinical use. Compounds that bi
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
