Dimeric 4-Aryl-1,4-Dihydropyridines: Development of a Third Class of Nonpeptidic HIV-1 Protease Inhibitors

Author(s): Andreas Hilgeroth .

Journal Name: Mini-Reviews in Medicinal Chemistry

Volume 2 , Issue 3 , 2002

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Cross-resistance development against most peptidic HIV-1 protease inhibitors (PI) forces the development of nonpeptidic alternatives. The classes of nonpeptidic protease inhibitors was limited so far to cyclic ureas and 4-hydroxy-2-pyrones with problems of limited bioavailability by extensive metabolism and protein binding. Cage dimeric 4-aryl-1,4-dihydropyridines have been developed as third class of nonpeptidic PIs. In the following synthesis, molecular modeling and biological activities of a first series of the novel PIs are reviewed. Bioavailability of the dimers will not be limited by protein binding and metabolism as far as evaluated.

Keywords: nonpeptide hiv inhibitor, nonpeptide pis, tipranavir

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Article Details

Year: 2002
Page: [235 - 245]
Pages: 11
DOI: 10.2174/1389557023406241
Price: $58

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