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Design, synthesis, X-ray studies, and biological evaluation of novel macrocyclic HIV-1 protease inhibitors involving the P1′–P2′ ligands
Design, synthesis, and evaluation of a new class of HIV-1 protease inhibitors containing diverse flexible macrocyclic P1′–P2′ tethers are reported. Inhibitor 5a with a pyrrolidinone-derived macrocycle exhibited favorable enzyme inhibitory and antiviral activity (K(i) = 13.2 nM, IC(50) = 22 nM). Furt...
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| Publicado no: | Bioorg Med Chem Lett |
|---|---|
| Main Authors: | , , , , , , , , , |
| Formato: | Artigo |
| Idioma: | Inglês |
| Publicado em: |
2017
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| Assuntos: | |
| Acesso em linha: | https://ncbi.nlm.nih.gov/pmc/articles/PMC5647257/ https://ncbi.nlm.nih.gov/pubmed/28958624 https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1016/j.bmcl.2017.09.003 |
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