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J Med Chem. 2002 Jul 18;45(15):3321-4.

Synthesis and antiviral activity of new anti-HIV amprenavir bioisosteres.

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Laboratoire de Chimie Biomoléculaire, Faculté des Sciences de Luminy, case 901, Université de la Méditerranée, 70 route Léon Lachamp, 13288 Marseille Cedex 9, France.


Starting from the chemical structure of the recent FDA-approved anti-HIV drug Amprenavir (Agenerase), a potent HIV-protease inhibitor, we have designed new series of Amprenavir bioisoteres in which the methylene group of the benzyl group was replaced by a sulfur atom. This structural modification has required an original multistep synthesis. Unfortunately, introduction of the sulfur atom abolished or drastically decreased both inhibitory activity on recombinant HIV protease and HIV infection protection on MT4 cell cultures.

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