Design, Synthesis and X-ray Structural Studies of Potent HIV-1 Protease Inhibitors Containing C-4 Substituted Tricyclic Hexahydro-furofuran derivatives as P2 ligands.
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DOI: 10.1002/cmdc.202200058
Abstract: The design, synthesis, X-ray structural, and biological evaluation of a series of highly potent HIV-1 protease inhibitors are reported herein. These inhibitors incorporated novel cyclohexane-fused tricyclic bis -tetrahydrofuran as P2 ligands in combination with a… read more here.
Keywords: synthesis ray; protease; potent hiv; hiv protease ... See more keywords
Discovery of novel piperidine-substituted indolylarylsulfones as potent HIV NNRTIs via structure-guided scaffold morphing and fragment rearrangement.
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DOI: 10.1016/j.ejmech.2016.10.009
Abstract: To further explore the chemical space around the entrance channel of HIV-1 reverse transcriptase (RT), a series of novel indolylarylsulfones (IASs) bearing N-substituted piperidine at indole-2-carboxamide were identified as potent HIV NNRTIs by structure-guided scaffold… read more here.
Keywords: scaffold morphing; structure guided; guided scaffold; hiv nnrtis ... See more keywords
Design and Synthesis of Potent HIV-1 Protease Inhibitors Containing Bicyclic Oxazolidinone Scaffold as the P2 Ligands: Structure-Activity Studies and Biological and X-ray Structural Studies.
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DOI: 10.1021/acs.jmedchem.8b01227
Abstract: We have designed, synthesized, and evaluated a new class of potent HIV-1 protease inhibitors with novel bicyclic oxazolidinone derivatives as the P2 ligand. We have developed an enantioselective synthesis of these bicyclic oxazolidinones utilizing a… read more here.
Keywords: potent hiv; protease; bicyclic oxazolidinone; protease inhibitors ... See more keywords
Novel diaryltriazines with a picolinonitrile moiety as potent HIV-1 RT inhibitors: a patent evaluation of WO2016059647(A2)
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DOI: 10.1080/13543776.2017.1262349
Abstract: ABSTRACT Diaryltriazine derivatives, which are structurally related to diarylpyrimidines, are a representative class of HIV-1 reverse transcriptase inhibitors with remarkable antiviral activities against wild-type and several mutant strains of HIV-1. A series of novel diaryltriazines… read more here.
Keywords: potent hiv; novel diaryltriazines; hiv; hiv inhibitors ... See more keywords
Structural Basis of 2-Phenylamino-4-phenoxyquinoline Derivatives as Potent HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitors
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DOI: 10.3390/molecules27020461
Abstract: New target molecules, namely, 2-phenylamino-4-phenoxyquinoline derivatives, were designed using a molecular hybridization approach, which was accomplished by fusing the pharmacophore structures of three currently available drugs: nevirapine, efavirenz, and rilpivirine. The discovery of disubstituted quinoline… read more here.
Keywords: phenoxyquinoline derivatives; potent hiv; phenylamino phenoxyquinoline; quinoline ... See more keywords