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Novel Pirfenidone Analogues: Synthesis of Pyridin‐2‐ones for the Treatment of Pulmonary Fibrosis
Author(s) -
Ammar Yousry A.,
Ismail Magda M. F.,
ElSehrawi Hend M.,
Noaman Eman,
Bayomi Ashraf H.,
Shawer Taghreed Z.
Publication year - 2006
Publication title -
archiv der pharmazie
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.468
H-Index - 61
eISSN - 1521-4184
pISSN - 0365-6233
DOI - 10.1002/ardp.200600017
Subject(s) - pirfenidone , hydroxyproline , chemistry , bicyclic molecule , pyrimidine , pyridine , bleomycin , stereochemistry , idiopathic pulmonary fibrosis , combinatorial chemistry , medicinal chemistry , lung , biochemistry , medicine , chemotherapy
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 μmol/lung, respectively. However, bicyclic pyridone VIIIb displayed a high mortality rate. Detailed syntheses, spectroscopic and biological data are reported.