Synthesis and analgesic action of N-(substituted-ethyl)pyrrole-3,4-dicarboximides

Add time:08/03/2019    Source:sciencedirect.com

We prepared a series of new N-[2-(4-substitutedpiperazin-1-yl)ethyl]-1-(n-butyl or phenyl)-2,5-dimethyl-3,4-pyrroledicarboximides 3 and the related products 4 and 5, nine representatives of which were evaluated as potential analgesic agents in an animal model (mice). The new pyrroledicarboximides were not toxic (LD50 ≥ 1466 mg/kg) and eight of them displayed analgesic activity ~1.5–5 times superior to that of ASA in the writhing test. However, the compounds were found to be unstable in methanol solution and in dilute bases (methanol/NaOMe). The S–A relationship is discussed.

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