79094-20-5Relevant articles and documents
Thromboxane A2 receptor antagonists. Synthesis and activities of phenylsulfonamido derivatives
Mais, DE,Mohamadi, F,Dube, GP,Kurtz, WL,Brune, KA,et al.
, p. 821 - 827 (2007/10/02)
A number of phenylsulfonamido derivatives have been synthesized and tested for their ability to inhibit: a) thromboxane A2/prostaglandin H2 (TXA2/PGH2) mimetic (U46619)-induced guinea pig platelet aggregation; b) aortic ring contraction; and c) binding of a radioiodinated TXA2/PGH2 mimetic (I-BOP) to platelets.In platelets, Kd values ranged from 9 nM to > 50 μM. pKb values in aortic rings ranged from 7.63 to 3.66 and in platelets from 7.7 to A high degree of correlation was observed between the Kd and pKb values found in the 3 sytems.Antagonist activity at the TXA2/PGH2 receptor was sensitive to both the substitution pattern of the 2 aromatic rings and the presence of heteroatoms.For 2 of the derivatives (4 and 11) molecular mechanics calculations were performed which indicated subtle structural differences that may account for the > 300-fold difference in potency observed for these analogs at the platelet TXA2/PGH2 receptor. thromboxane A2 / antagonist / platelet / artery / receptor / phenylsulfonamido derivative