Synthesis and pharmacological screening of some N-(4-substituted-piperazin-1-ylalkyl)-3,4-pyrroledicarboximides

As an extension of our previous work we describe the synthesis and pharmaco logical investigation of a new series of derivatives of pyrrole-3,4-dicarbo ximide possessing the 4-substitutecl-piperazin-1-ylalkyl group linked to th e imide nitrogen. The products were-evaluated for acute toxicity, and effec tiveness in a series of CNS and arterial blood pressure tests. The prelimin ary pharmacological screening was determined in animal models. Several comp ounds demonstrated moderate to high analgesic activity in the 'writhing syn drome' test (5f-1/640 LD50). Some of the structure-activity relationships a re also discussed. (C) 1999 Elsevier Science S.A. All rights reserved.