Synthesis and Biological Activity of 4-(Diphenylmethyl)-α--1-piperazineethanol and Related Compounds

Article abstract of DOI:10.1021/jm00101a022

A series of 4-(diphenylmethyl)-α-<(4-quinolinyloxy)methyl>-1-piperazineethanol and closely related compounds was synthesised and evaluated for cardiac and vascular activity in isolated perfused rat and guinea pig hearts.Compound 1 produced greater inotropic effects in rat hearts than in guinea pig hearts, a phenomenon which was also observed with the prototype agent DPI 201-106.Compound 15 produced an inotropic effect with one-tenth the potency of compound 1.Both compounds 1 and 15 demonstrated direct inotropic and vasodilatory effects when administered iv in anesthetized dogs, although the vasodilatory activity was more pronounced with compound 15 than 1 and DPI compound.Compound 1 lacks the CN moiety which is a key structural requirement in DPI for positive inotropic activity.The synthesis, in vitro, and in vivo evaluations of these agents, and comparative data with DPI-201-106 (compound 17) are reported.