1001289-58-2Relevant academic research and scientific papers
Evaluation and optimization of antifibrotic activity of cinnamoyl anthranilates
Zammit, Steven C.,Cox, Alison J.,Gow, Renae M.,Zhang, Yuan,Gilbert, Richard E.,Krum, Henry,Kelly, Darren J.,Williams, Spencer J.
supporting information; experimental part, p. 7003 - 7006 (2010/07/08)
Tranilast is an anti-inflammatory drug in use for asthma and atopic dermatitis. In studies over the last decade it has been revealed that tranilast can reduce fibrosis occurring in the kidney during diabetes, thereby delaying and/or preventing kidney dysfunction. We report a structure-activity study aimed at optimizing the antifibrotic activity of tranilast. A series of cinnamoyl anthranilates were prepared and assessed for their ability to prevent TGF-β-stimulated production of collagen in cultured renal mesangial cells. We reveal derivatives with improved potency and reduced cellular toxicity relative to tranilast. 3-Methoxy-4-propargyloxycinnamoyl anthranilate reduces albuminuria in a rat model of progressive diabetes, and thus has potential as an innovative treatment for diabetic nephropathy.
THERAPEUTIC COMPOUNDS
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Page/Page column 71, (2008/06/13)
Substituted cinnamoyl anthranilate compounds exhibiting anti-fibrotic activity; or derivatives thereof, analogues thereof, pharmaceutically acceptable salts thereof, and metabolites thereof; with the proviso that the compound is not Tranilast.
