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Halogen Bond Interactions of Novel HIV-1 Protease Inhibitors (PI) (GRL-001-15 and GRL-003-15) with the Flap of Protease Are Critical for Their Potent Activity against Wild-Type HIV-1 and Multi-PI-Resistant Variants

We generated two novel nonpeptidic HIV-1 protease inhibitors (PIs), GRL-001-15 and GRL-003-15, which contain unique crown-like tetrahydropyranofuran (Crn-THF) and P2′-cyclopropyl-aminobenzothiazole (Cp-Abt) moieties as P2 and P2′ ligands, respectively. GRL-001-15 and GRL-003-15 have meta-monofluorop...

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Detalhes bibliográficos
Publicado no:Antimicrob Agents Chemother
Main Authors: Hattori, Shin-ichiro, Hayashi, Hironori, Bulut, Haydar, Rao, Kalapala Venkateswara, Nyalapatla, Prasanth R., Hasegawa, Kazuya, Aoki, Manabu, Ghosh, Arun K., Mitsuya, Hiroaki
Formato: Artigo
Idioma:Inglês
Publicado em: American Society for Microbiology 2019
Assuntos:
Acesso em linha:https://ncbi.nlm.nih.gov/pmc/articles/PMC6535520/
https://ncbi.nlm.nih.gov/pubmed/30962341
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1128/AAC.02635-18
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