Novel Pirfenidone Analogues: Synthesis of Pyridin‐2‐ones for the Treatment of Pulmonary Fibrosis | Zendy

Ammar Yousry A. | Zendy; Ismail Magda M. F. | Zendy; ElSehrawi Hend M. | Zendy; Noaman Eman | Zendy; Bayomi Ashraf H. | Zendy; Shawer Taghreed Z. | Zendy

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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.

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