Literature DB >> 2724294

Synthesis and antiinflammatory and analgesic activity of 5-aroyl-6-(methylthio)-1,2-dihydro-3H-pyrrolo[1,2-a]pyrrole-1-ca rboxyl ic acids and 1-methyl-4-(methylthio)-5-aroylpyrrole-2-acetic acids.

J M Muchowski1, E Galeazzi, R Greenhouse, A Guzmán, V Peréz, N Ackerman, S A Ballaron, J R Rovito, A J Tomolonis, J M Young.   

Abstract

5-Aroyl-6-(methylthio)-1,2-dihydro-3H-pyrrolo[1,2-a]pyrrole-1-carb oxylic acids and 1-methyl-4-(methylthio)-5-aroylpyrrole-2-acetic acids were synthesized and assayed as antiinflammatory and analgesic agents. The majority of these compounds exhibit a surprisingly low level of antiinflammatory activity (rat carrageenan paw) but have considerable potency as analgesics (mouse phenylquinone writing). For example, the p-tolyl-substituted bicyclic and monocyclic compounds 44 and 58 are 301 and 66 times more potent than aspirin (mouse writhing) but only 3.4 and 1.5 times more potent than phenylbutazone in the antiinflammatory screen (rat paw).

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Year:  1989        PMID: 2724294     DOI: 10.1021/jm00126a010

Source DB:  PubMed          Journal:  J Med Chem        ISSN: 0022-2623            Impact factor:   7.446


  1 in total

1.  A New Synthetic Route to Polyhydrogenated Pyrrolo[3,4-b]pyrroles by the Domino Reaction of 3-Bromopyrrole-2,5-Diones with Aminocrotonic Acid Esters.

Authors:  Khidmet Shikhaliev; Artem Sabynin; Valeri Sekirin; Michael Krysin; Fedor Zubkov; Kristina Yankina
Journal:  Molecules       Date:  2017-11-22       Impact factor: 4.411

  1 in total

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