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. 2006 Aug;339(8):429-36.
doi: 10.1002/ardp.200600017.

Novel pirfenidone analogues: synthesis of pyridin-2-ones for the treatment of pulmonary fibrosis

Yousry A Ammar  1 , Magda M F Ismail, Hend M El-Sehrawi, Eman Noaman, Ashraf H Bayomi, Taghreed Z Shawer
Affiliations

Novel pirfenidone analogues: synthesis of pyridin-2-ones for the treatment of pulmonary fibrosis

Yousry A Ammar et al. Arch Pharm (Weinheim). 2006 Aug.

Abstract

A new series of polysubstituted 1-aryl-2-oxo-1,2-dihydropyridine-3-carbonitriles and pyrazolo[3,4-b]pyridine-5-carbonitriles and pyrido[2,3-d]pyrimidine-6-carbonitriles have been synthesized and tested for their antifibrotic activity. Among the tested compounds, compounds IIc and IVb exhibited higher antifibrotic activity than the standard pirfenidone PD with a reduction of the hydroxyproline level to 50 and 140 micromol/lung, respectively. However, bicyclic pyridone VIIIb displayed a high mortality rate. Detailed syntheses, spectroscopic and biological data are reported.

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