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Synthesis, antiinflammatory and analgesic activity of 5-aroyl-1, 2-dihydro-3H-pyrrolo [1, 2-a] pyrrole-1-carboxylic acids and related compounds

…, P Cheung, J Cook, P Gallegra, O Halpern…

文献索引:Muchowski; Unger; Ackrell; Cheung; Cooper; Cook; Gallegra; Halpern; Koehler; Kluge Journal of Medicinal Chemistry, 1985 , vol. 28, # 8 p. 1037 - 1049

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被引用次数: 68

摘要

5-Acyl-l, 2-dihydro-3H-pyrrolo [1, 2-a] pyrrole-l-carboxylic acids and the homologous pyridine and azepine derivatives were synthesized and assayed for antiinflammatory and analgesic activity. 5-Benzoyl-l, 2-dihydro-3H-pyrrolo-[1, 2-a] pyrrole-l-carboxylic acid (62) and the corresponding p-methoxy compound 74 were selected for evaluation as analgesic agents in humans on the basis of their high potency in the mouse phenylquinone writhing ...