Design, synthesis, and evaluation of diarylpyridines and diarylanilines as potent non-nucleoside HIV-1 reverse transcriptase inhibitors. [PDF]
J Med Chem, 2010 Based on the structures and activities of our previously identified non-nucleoside reverse transcriptase inhibitors (NNRTIs), we designed and synthesized two sets of derivatives, diarylpyridines (A) and diarylanilines (B), and tested their anti-HIV-1 ...
Tian X +9 more
europepmc +3 more sources
Application of 3D-QSAR, Pharmacophore, and Molecular Docking in the Molecular Design of Diarylpyrimidine Derivatives as HIV-1 Nonnucleoside Reverse Transcriptase Inhibitors. [PDF]
Int J Mol Sci, 2018 Diarylpyrimidines (DAPYs), acting as HIV-1 nonnucleoside reverse transcriptase inhibitors (NNRTIs), have been considered to be one of the most potent drug families in the fight against acquired immunodeficiency syndrome (AIDS).
Liu G, Wang W, Wan Y, Ju X, Gu S.
europepmc +2 more sources
Design, synthesis, and preclinical evaluations of novel 4-substituted 1,5-diarylanilines as potent HIV-1 non-nucleoside reverse transcriptase inhibitor (NNRTI) drug candidates. [PDF]
J Med Chem, 2012 Twenty-one new 4-substituted diarylaniline compounds (DAANs) (Scheme 2, series 13, 14, and 15) were designed, synthesized, and evaluated against wild-type and drug resistant HIV-1 viral strains.
Sun LQ +7 more
europepmc +3 more sources
Optimization of the antiviral potency and lipophilicity of halogenated 2,6-diarylpyridinamines as a novel class of HIV-1 NNRTIS. [PDF]
ChemMedChem, 2014 Nineteen new halogenated diarylpyridinamine (DAPA) analogues (6a-n and 8a-e) modified on the phenoxy C-ring were synthesized and evaluated for anti-HIV activity and certain drug-like properties. Ten compounds showed high anti-HIV activity (EC50 0.3, LLE
Wu ZY +10 more
europepmc +3 more sources
Diarylaniline derivatives as a distinct class of HIV-1 non-nucleoside reverse transcriptase inhibitors. [PDF]
J Med Chem, 2010 By using structure-based drug design and isosteric replacement, diarylaniline and 1,5-diarylbenzene-1,2-diamine derivatives were synthesized and evaluated against wild type HIV-1 and drug-resistant viral strains, resulting in the discovery of ...
Qin B +11 more
europepmc +3 more sources
Bioorganic and Medicinal Chemistry, 2017 30 new analogues of diarylpyrimidines were synthesized for further structural modifications, involving not only the linker but also the wing α of DAPYs.
Yuan-Yuan Zhu +2 more
exaly +3 more sources
European 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 ...
Christophe Pannecouque +2 more
exaly +2 more sources
Privileged scaffold inspired design of novel oxime-biphenyl-DAPYs in treatment of HIV-1
Bioorganic 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).
Christophe Pannecouque +2 more
exaly +2 more sources
Bioorganic 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.
Hu-Ri Piao, Fen-Er Chen, Erik De Clercq
exaly +2 more sources
Bioorganic 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 ...
Shuang-Xi Gu +2 more
exaly +2 more sources