Abstract
A series of novel cinnamoylpiperazine derivatives (5a–5l) were synthesized as potential antinociceptive, and anticonvulsive agents. Various heterocyclic systems like piperidine, morpholine, piperazine, and N-arylpiperazine were combined with cinnamoyl or methylenedioxy cinnamoyl moieties to obtain a series of constrained analogs of cinnamides. Of these, compound 5e possessing 4-fluorophenyl substitution on the piperazine ring exhibited good antinociceptive activity in capsaicin and formalin-induced nociception methods, and also significant anticonvulsant activity in pentylenetetrazole and maximal electroshock-induced seizure methods. Further, all the derivatives were studied for molecular and preadmet properties. The activities of compound 5e were supported by molecular and preadmet properties for its in silico oral bioavailability and drug-likeness.
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Prasanthi, G., Prasad, K. & Bharathi, K. Synthesis, evaluation, and molecular properties prediction of substituted cinnamoylpiperazine derivatives as potential antinociceptive and anticonvulsive agents. Med Chem Res 27, 1599–1608 (2018). https://doi.org/10.1007/s00044-018-2175-z
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DOI: https://doi.org/10.1007/s00044-018-2175-z