, 2022 A series of novel heteroaromatic biphenyl-methyl-pyrimidine analogues were designed via hybridization of privileged structures of two HIV-1 inhibitors.
Li Ding +4 more
core +8 more sources
Structural Studies and Structure Activity Relationships for Novel Computationally Designed Non-nucleoside Inhibitors and Their Interactions With HIV-1 Reverse Transcriptase. [PDF]
Front Mol Biosci, 2022 Reverse transcriptase (RT) from the human immunodeficiency virus continues to be an attractive drug target for antiretroviral therapy. June 2022 will commemorate the 30th anniversary of the first Human Immunodeficiency Virus (HIV) RT crystal structure ...
Frey KM +7 more
europepmc +3 more sources
, 2017 30 new analogues of diarylpyrimidines were synthesized for further structural modifications, involving not only the linker but also the wing α of DAPYs.
Huan-Huan Lu +9 more
core +3 more sources
Focus on Chirality of HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitors. [PDF]
Molecules, 2016 Chiral HIV-1 non-nucleoside reverse transcriptase inhibitors (NNRTIs) are of great interest since one enantiomer is often more potent than the corresponding counterpart against the HIV-1 wild type (WT) and the HIV-1 drug resistant mutant strains.
Famiglini V, Silvestri R.
europepmc +4 more sources
Privileged scaffold inspired design of novel oxime-biphenyl-DAPYs in treatment of HIV-1 [PDF]
, 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).
Yang Yang +4 more
openalex +2 more sources
, 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 +8 more
openalex +3 more sources
, 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.
Zihong Yan +7 more
openalex +2 more sources
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
Synthetic Approaches for Pharmacologically Active Decorated Six-Membered Diazines [PDF]
, 2022 Diazine alkaloid (pyridazine, pyrimidine and pyrazine) scaffold, a widespread two-nitrogen containing compounds in nature (DNA, RNA, flavors, and fragrances), constitutes a central building block for wide range of pharmacological applications.
Khoury, Maha Awwad, Najajreh, Yousef
core +2 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