Results 81 to 90 of about 148 (100)

Discovery of Novel Pyridine-Dimethyl-Phenyl-DAPY Hybrids by Molecular Fusing of Methyl-Pyrimidine-DAPYs and Difluoro-Pyridinyl-DAPYs: Improving the Druggability Toward High Inhibitory Activity, Solubility, Safety, and PK

open access: yesJournal of Medicinal Chemistry, 2022
A series of novel heteroaromatic biphenyl-methyl-pyrimidine analogues were designed via hybridization of privileged structures of two HIV-1 inhibitors.
Chunlin Zhuang   +2 more
exaly   +7 more sources

Fragment Hopping-Based Discovery of Novel Sulfinylacetamide-Diarylpyrimidines (DAPYs) as HIV-1 Nonnucleoside Reverse Transcriptase Inhibitors

open access: yesEuropean Journal of Medicinal Chemistry, 2020
The fragment hopping approach is widely applied in drug development. A series of diarylpyrimidines (DAPYs) were obtained by hopping the thioacetamide scaffold to novel human immunodeficiency virus type 1 (HIV-1) nonnucleoside reverse transcriptase ...
Chunlin Zhuang   +2 more
exaly   +2 more sources

Privileged Scaffold Inspired Design of Novel Oxime-Biphenyl-DAPYs in Treatment of HIV-1 [PDF]

open access: yesBioorganic Chemistry, 2020
Oxime is a key pharmacophore in drug development. The biphenyl diarylpyrimidines (DAPYs) have been developed by our group as novel non-nucleoside reverse transcriptase inhibitors (NNRTIs).
Chunlin Zhuang   +2 more
exaly   +2 more sources

Follow On-Based Optimization of the Biphenyl-DAPYs as HIV-1 Nonnucleoside Reverse Transcriptase Inhibitors Against the Wild-Type and Mutant Strains

open access: yesBioorganic Chemistry, 2019
The present work follows our preliminary discovery of biphenyl diarylpyrimidines (DAPYs) as HIV-1 nonnucleoside reverse transcriptase inhibitors. Further structural optimization of biphenyl-DAPYs led to the identification of a new series of biphenyl ...
Chunlin Zhuang   +2 more
exaly   +2 more sources

Synthesis and Biological Evaluation of CHX-DAPYs as HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitors

open access: yesBioorganic and Medicinal Chemistry, 2014
A series of new diarylpyrimidines (DAPYs) characterized by a halogen atom on the methylene linker between wing I and the central pyrimidine ring was synthesized and evaluated for their anti-HIV activity in MT-4 cell cultures.
Christophe Pannecouque   +2 more
exaly   +2 more sources

A Novel Family of Diarylpyrimidines (DAPYs) Featuring a Diatomic Linker: Design, Synthesis and Anti-HIV Activities

open access: yesBioorganic and Medicinal Chemistry, 2015
To improve the conformational flexibility and positional adaptability of the traditional diarylpyrimidines (DAPYs), a family of diarylpyrimidines featuring a C-N diatomic linker between the left wing benzene ring and the central pyrimidine was firstly ...
Christophe Pannecouque   +2 more
exaly   +2 more sources

Structural Modifications of Diarylpyrimidines (DAPYs) as HIV-1 NNRTIs: Synthesis, Anti-HIV Activities and SAR

open access: yesBioorganic and Medicinal Chemistry, 2017
30 new analogues of diarylpyrimidines were synthesized for further structural modifications, involving not only the linker but also the wing alpha of DAPYs.
Christophe Pannecouque   +2 more
exaly   +2 more sources

Discovery of Uracil-Bearing DAPYs Derivatives as Novel HIV-1 NNRTIs via Crystallographic Overlay-Based Molecular Hybridization

open access: yesEuropean Journal of Medicinal Chemistry, 2017
A novel series of uracil-bearing DAPYs derivatives were designed and synthesized via structure-based molecular hybridization to discover compounds with improved anti-resistance profiles. Anti-HIV activity of the designed compounds was tested in MT-4 cell
Zhongxia Zhou, Huiqing Liu, Dongwei Kang
exaly   +2 more sources

Structural Modifications of CH(OH)-DAPYs as New HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitors

open access: yesBioorganic and Medicinal Chemistry, 2014
A series of CR2(OH)-diarylpyrimidine derivatives (CR2(OH)-DAPYs) featuring a hydrophobic group at CH(OH) linker between wing I and the central pyrimidine were synthesized and evaluated for their anti-HIV activity in MT-4 cell cultures.
Christophe Pannecouque   +2 more
exaly   +2 more sources

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