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Probing Lipophilic Adamantyl Group as the P1-Ligand for HIV-1 Protease Inhibitors: Design, Synthesis, Protein X-ray Structural Studies, and Biological Evaluation

A series of potent HIV-1 protease inhibitors with a lipophilic adamantyl P1 ligand have been designed, synthesized and evaluated. We have developed an enantioselective synthesis of adamantane-derived hydroxyethylamine isostere utilizing Sharpless asymmetric epoxidation as the key step. Various inhib...

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Detalhes bibliográficos
Publicado no:J Med Chem
Main Authors: Ghosh, Arun K., Osswald, Heather L., Glauninger, Kristof, Agniswamy, Johnson, Wang, Yuan-Fang, Hayashi, Hironori, Aoki, Manabu, Weber, Irene T., Mitsuya, Hiroaki
Formato: Artigo
Idioma:Inglês
Publicado em: 2016
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Acesso em linha:https://ncbi.nlm.nih.gov/pmc/articles/PMC5360270/
https://ncbi.nlm.nih.gov/pubmed/27389367
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acs.jmedchem.6b00639
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