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Synthesis of Potent and Orally Active HIV‐Protease Inhibitors

 

作者: Hans‐Georg Capraro,   Guido Bold,   Alexander Fässler,   Robert Cozens,   Thomas Klimkait,   Janis Lazdins,   Jürgen Mestan,   Bernard Poncioni,   Johannes L. Rösel,   David Stover,   Marc Lang,  

 

期刊: Archiv der Pharmazie  （WILEY Available online 1996）
卷期: Volume 329, issue 6  

页码: 273-278

 

ISSN:0365-6233

 

年代: 1996

 

DOI:10.1002/ardp.19963290602

 

出版商: WILEY‐VCH Verlag

 

关键词: HIV‐1 protease;CGP 61755;Phe‐C‐Phe hydroxyethylene mimic

 

数据来源: WILEY

 

摘要:

AbstractA series of potent HIV‐protease inhibitors has been prepared. Several of the newly synthesized compounds showed high plasma levels after oral administration to animals. Based on the overall biological profile, CGP 61755 was chosen for further preclinical evaluation. For this compound, a 10 step synthesis potentially suitable for large scale production was develope

 

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