Synthesis and antiinflammatory and analgesic activity of 5-aroyl-1,2-dihydro-3H-pyrrolo[1,2-a]pyrrole-1-carboxylic acids. The 6-substituted compounds

5-Aroyl-6-substituted-1,2-dihydro-3H-pyrrolo[1,2-a]pyrrole-1-carbo xylic acids were synthesized and assayed for analgesic and antiinflammatory activity. Several of these compounds, notably the 5-(4-fluoro- and 4-chlorobenzoyl)-6-methyl derivatives 25 and 26 and the 5-(4-methyl-, 4-fluoro-, 4-chloro-...

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Bibliographic Details
Published in:Journal of medicinal chemistry 1987-05, Vol.30 (5), p.820-823
Main Authors: Muchowski, Joseph M, Cooper, Gary F, Halpern, Otto, Koehler, Richard, Kluge, Arthur F, Simon, Robert L, Unger, Stefan H, Van Horn, Albert R, Wren, Douglas L
Format: Article
Language:English
Subjects:
Analgesia
Animals
Carboxylic Acids - chemical synthesis
Carboxylic Acids - therapeutic use
Chemical Phenomena
Chemistry
Exact sciences and technology
Heterocyclic compounds
Heterocyclic compounds with only one n hetero atom and condensed derivatives
Inflammation - drug therapy
Magnetic Resonance Spectroscopy
Mice
Organic chemistry
Preparations and properties
Pyrroles - chemical synthesis
Pyrroles - therapeutic use
Rats
Structure-Activity Relationship
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Summary:5-Aroyl-6-substituted-1,2-dihydro-3H-pyrrolo[1,2-a]pyrrole-1-carbo xylic acids were synthesized and assayed for analgesic and antiinflammatory activity. Several of these compounds, notably the 5-(4-fluoro- and 4-chlorobenzoyl)-6-methyl derivatives 25 and 26 and the 5-(4-methyl-, 4-fluoro-, 4-chloro-, and 4-methoxybenzoyl)-6-chloro congeners 31-34 were of equal or greater potency than indomethacin as antiinflammatory and analgesic agents both in acute and chronic animal models.
ISSN:0022-2623
1520-4804
DOI:10.1021/jm00388a013