Molecular design and synthesis of 1,4-disubstituted piperazines as α1-adrenergic receptor blockers

Add time:08/09/2019    Source:sciencedirect.com

A new series of 4,5,6,7-tetrahydrothieno[2,3-c]pyridine-3-carboxylic acid amide and 3,5,6,8-tetrahydropyrido[4′,3′:4,5]thieno[2,3-d]pyrimidin-4-one derivatives were designed, synthesized, their binding and functional properties as α1-adrenoreceptors blockers were evaluated. A new validated α1-adrenoreceptor blocker pharmacophore model (hypothesis) was generated using Discovery Studio 2.5. The compare-fit study for the designed molecules with the generated hypothesis was fulfilled and several compounds showed significant high fit values. Compounds IVa–c, VIIa–d, VIIIa–c, Xa–c, XIa–d have shown blocking activity ranging from 46.73% up to 94.74% compared to 99.17% for prazosin.

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