Trimetoquinol [TMQ] is a nonspecific beta-adrenergic agonist, as well as a competitive inhibitor of human platelet aggregation and rat aortic contraction induced by the TXA2 mimetic, U46619.
TXA2/PHG2 receptors have been subclassified as the platelet alpha receptor [aggregation] and the vascular alpha receptor [contractile responses] . It was found that 5- and 8-fluoro TMQ have a greater beta 2/beta 1 selectivity ratio than TMQ and also selectively inhibit U46619 action on aorta versus platelets. To study the optimal structure activity relationships for TMQ analogs with respect to improving the beta 2/beta 1 selectivity ratio and to separate alpha vs tau TXA2/PHG2 inhibitory activity, 5, 8-difluoro TMQ and the synthetic approaches to 5-trifluoromethyl and 8-trifluoromethyl TMQ were prepared, and their biological activities were reported
K. M. Markovich ,
Synthesis and biological activities of 5, 8-difluorotrimetoquinol and synthetic approaches to trifluoromethyl analogs of trimetoquinol,
Egypt. J. Pharm. Sci. 1994;
411-418 Views : 0