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• W2805018614 abstract "The design, synthesis, and biological evaluation of a new class of HIV-1 protease inhibitors containing stereochemically defined fused tricyclic polyethers as the P2 ligands and a variety of sulfonamide derivatives as the P2' ligands are described. A number of ring sizes and various substituent effects were investigated to enhance the ligand-backbone interactions in the protease active site. Inhibitors 5c and 5d containing this unprecedented fused 6-5-5 ring system as the P2 ligand, an aminobenzothiazole as the P2' ligand, and a difluorophenylmethyl as the P1 ligand exhibited exceptional enzyme inhibitory potency and maintained excellent antiviral activity against a panel of highly multidrug-resistant HIV-1 variants. The umbrella-like P2 ligand for these inhibitors has been synthesized efficiently in an optically active form using a Pauson-Khand cyclization reaction as the key step. The racemic alcohols were resolved efficiently using a lipase catalyzed enzymatic resolution. Two high resolution X-ray structures of inhibitor-bound HIV-1 protease revealed extensive interactions with the backbone atoms of HIV-1 protease and provided molecular insight into the binding properties of these new inhibitors." @default.
• W2805018614 created "2018-06-01" @default.
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• W2805018614 date "2018-05-15" @default.
• W2805018614 modified "2023-10-06" @default.
• W2805018614 title "Design and Synthesis of Highly Potent HIV-1 Protease Inhibitors Containing Tricyclic Fused Ring Systems as Novel P2 Ligands: Structure–Activity Studies, Biological and X-ray Structural Analysis" @default.
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• W2805018614 doi "https://doi.org/10.1021/acs.jmedchem.8b00298" @default.
• W2805018614 hasPubMedCentralId "https://www.ncbi.nlm.nih.gov/pmc/articles/6044451" @default.
• W2805018614 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/29763303" @default.
• W2805018614 hasPublicationYear "2018" @default.
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