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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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Bibliografske podrobnosti
izdano v:Bioorg Med Chem Lett
Main Authors: Ghosh, Arun K., Fyvie, W. Sean, Brindisi, Margherita, Steffey, Melinda, Agniswamy, Johnson, Wang, Yuan-Fang, Aoki, Manabu, Amano, Masayuki, Weber, Irene T., Mitsuya, Hiroaki
Format: Artigo
Jezik:Inglês
Izdano: 2017
Teme:
Online dostop: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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