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Development of Synthetic Strategies for the Construction of Pyrido[4,3‐ d ]pyrimidine Libraries – the Discovery of a New Class of PDE‐4 Inhibitors
Author(s) -
Jang MiYeon,
De Jonghe Steven,
Gao LingJie,
Rozenski Jef,
Herdewijn Piet
Publication year - 2006
Publication title -
european journal of organic chemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.825
H-Index - 155
eISSN - 1099-0690
pISSN - 1434-193X
DOI - 10.1002/ejoc.200600339
Subject(s) - chemistry , pyrimidine , scaffold , combinatorial chemistry , stereochemistry , drug discovery , class (philosophy) , biochemistry , computer science , programming language , artificial intelligence
The synthesis of a pyrido[4,3‐ d ]pyrimidine library from 4,6‐diamino‐2‐bromonicotinamide and 4,6‐diaminonicotinamide is described. A systematic variation of the substituents at positions 2, 4, 5 and 7 of the pyrido[4,3‐ d ]pyrimidine scaffold was carried out, leading to a wide variety of structural analogues. This strategy led to the discovery of a new structural class of PDE‐4 inhibitors. (© Wiley‐VCH Verlag GmbH & Co. KGaA, 69451 Weinheim, Germany, 2006)