169298-35-5Relevant articles and documents
Synthesis and evaluation of novel fluorinated sulotroban-related sulfonamide derivatives as thromboxane A2 receptor antagonists
Sato,Kawashima,Goto,Yamane,Chiba,Jinno,Satake,Iwata
, p. 403 - 414 (2007/10/02)
A series of sulotroban-related arylsulfonamide derivatives possessing a fluorinated phenoxyacetic acid moiety was synthesized and tested for TXA2 antagonizing ability on U-46619-induced platelet aggregation of rabbit platelet-rich plasma. Introduction of one or more fluorine atoms to the phenoxyacetic acid moiety increased this activity. The most potent compound among these compounds was 10c, which was 40-fold more potent (IC50 3.4 x 10-7 M) than sulotroban. 10c exhibited high activity (ID50 0.14 mg/kg) against a D-46619-induced acute thrombocytopenia model in mice when orally administrated. These findings and those of radioligand binding assays with various ligands showed 10c to be a potent and selective systemic TXA2 receptor antagonist.