Abstract
Mannich bases obtained by aminoalkylation of 3 H-pyrrolo[3,2- f]quinoline were designed and prepared as potential vasorelaxing agents. Compounds Ia– Va were characterised by IR, 1H-NMR, mass spectral data and elemental analysis; IIb, c– Vb, c were also confirmed by 1H-NMR spectra of reaction mixtures. To estimate their vascular activity, prototypes 1-( N, N-dimethylaminomethyl)- ( Ia) and 1-(4-phenyl-piperazin-1-ylmethyl)- ( IVa) 3 H-pyrrolo[3,2- f]quinoline derivatives were studied in rat-tail arteries. In tissues precontracted with 0.5 μM 5-hydroxytryptamine (5-HT), 3 μM phenylephrine or 80 mM KCl, Ia and IVa showed endothelium-independent relaxing action. In a preliminary study on the cellular mechanisms of Ia, the influence of propranolol, a β-receptor antagonist, and ketanserin, a 5-HT 2A-receptor antagonist, was checked. In the presence of phenylephrine, the vasorelaxing effect of Ia was not affected by these inhibitors.
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