Journal of Medicinal Chemistry p. 4442 - 4449 (1992)
Update date:2022-09-26
Topics:
Sircar, Ila
Haleen, Steve J.
Burke, Sandra E.
Barth, Hubert
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.
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Doi:10.1021/ja4046857
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(1992)Doi:10.1021/jm400405z
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(1992)