76786-67-9Relevant academic research and scientific papers
Synthesis and antiinflammatory and analgesic activity of 5-aroyl-1,2-dihydro-3H-pyrrolo[1,2-a]pyrrole-1-carboxylic acids and related compounds
Muchowski,Unger,Ackrell,Cheung,Cooper,Cook,Gallegra,Halpern,Koehler,Kluge
, p. 1037 - 1049 (2007/10/02)
5-Acyl-1,2-dihydro-3H-pyrrolo[1,2-a]pyrrole-1-carboxylic acids and the homologous pyridine and azepine derivatives were synthesized and assayed for antiinflammatory and analgesic activity. 5-Benzoyl-1,2-dihydro-3H-pyrrolo-[1,2-a]pyrrole-1-carboxylic acid and the corresponding p-methoxy compound were selected for evaluation as analgesic agents in humans on the basis of their high potency in the mouse phenylquinone writhing assay as well as on their minimal liability to elicit gastrointestinal erosion in rats on chronic administration. Extensive quantitative structure-activity relationship (QSAR) studies of the benzoylpyrrolopyrrolecarboxylic acids have demonstrated that the analgesic (mouse writhing) and antiinflammatory (rat carrageenan paw) potencies of these compounds are satisfactorily correlated with the steric and hydrogen-bonding properties of the benzoyl substituent(s). The 4-vinylbenzoyl compound, which was correctly predicted to be highly active in both assays on this basis, is undergoing advanced pharmacological evaluation in animals as a potential antiinflammatory agent.
Use of pyrrolo pyrroles in treatment of ophthalmic diseases
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, (2008/06/13)
Certain known pyrroles have been found to be useful in the topical treatment of various ophthalmic diseases in mammals; especially those originating from or associated with inflammation such as, for example, cystoid macular edema, glaucoma, conjunctivitis, uveitis, diabetic retinopathy and eye surgery or trauma.
Use of pyrrolo-pyrrole in treating microvascular diseases associated with diabetes
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, (2008/06/13)
The present invention concerns a new use of certain pyrrolo-pyrrole compounds of chemical formulas (A), (B), (C), and (D): STR1 for the treatment of microvascular complications associated with diabetes such as, for example, diabetic retinopathy, diabetic nephropathy and diabetic neuropathy. Pyrrolo-pyrrole compounds prevent development, restrain further progress and relieve symptoms of already developed microvascular complications of diabetes.
