The condensation of asymmetrically substituted 1,4-bis(haloacyl) piperazines with secondary amines yielded asymmetric 1,4-bis (aminoacyl) piperazines 3-6, which were further transformed into the respective dimethiodides 3b-6b by treatment with methyl iodide. Those compounds were found to inhibit the neuromuscular transmission by blocking the motor end-plate receptors. Compounds containing piperidine moiety and branched acyl chain 4b displayed enhanced activity.

Asymmetric 1,4-bis(aminoacyl) piperazines inhibit neuromuscular transmission by blocking motor end-plate receptors, with compounds containing piperidine moiety and branched acyl chain showing enhanced activity.

Paper

Synthesis and effect of asymmetric 1,4-bis(aminoacyl) piperazines on neuromuscular transmission.

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