Scaffold Hopping in Discovery of HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitors: From CH(CN)-DABOs to CH(CN)-DAPYs [PDF]
Molecules, 2020 Scaffold hopping is a frequently-used strategy in the development of non-nucleoside reverse transcriptase inhibitors. Herein, CH(CN)-DAPYs were designed by hopping the cyano-methylene linker of our previous published CH(CN)-DABOs onto the etravirine (ETR)
Christophe Pannecouque +2 more
exaly +7 more sources
Hydrogen Bonding (Base Pairing) in Antiviral Activity [PDF]
Viruses, 2023 Base pairing based on hydrogen bonding has, since its inception, been crucial in the antiviral activity of arabinosyladenine, 2′-deoxyuridines (i.e., IDU, TFT, BVDU), acyclic nucleoside analogues (i.e., acyclovir) and nucleoside reverse transcriptase ...
Erik De Clercq
doaj +2 more sources
Development of fluorine-substituted NH2-biphenyl-diarylpyrimidines as highly potent non-nucleoside reverse transcriptase inhibitors: Boosting the safety and metabolic stability [PDF]
Acta Pharmaceutica Sinica B, 2023 Our recent studies for nonnucleoside reverse transcriptase inhibitors identified a highly potent compound JK-4b against WT HIV-1 (EC50 = 1.0 nmol/L), but the poor metabolic stability in human liver microsomes (t1/2 = 14.6 min) and insufficient ...
Xin Jin +9 more
doaj +2 more sources
Picomolar inhibitor of reverse transcriptase featuring significantly improved metabolic stability [PDF]
Acta Pharmaceutica Sinica B, 2023 Considering the undesirable metabolic stability of our recently identified NNRTI 5 (t1/2 = 96 min) in human liver microsomes, we directed our efforts to improve its metabolic stability by introducing a new favorable hydroxymethyl side chain to the C-5 ...
Ya-Li Sang +4 more
doaj +2 more sources
Development of non-nucleoside reverse transcriptase inhibitors (NNRTIs): our past twenty years [PDF]
Acta Pharmaceutica Sinica B, 2020 Human immunodeficiency virus (HIV) is the primary infectious agent of acquired immunodeficiency syndrome (AIDS), and non-nucleoside reverse transcriptase inhibitors (NNRTIs) are the cornerstone of HIV treatment.
Chunlin Zhuang +3 more
doaj +2 more sources
Identification of Novel Diarylpyrimidines as Potent HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitors by Exploring the Primer Grip Region [PDF]
Pharmaceuticals, 2022 HIV-1 reverse transcriptase (RT) plays a crucial role in the viral replication cycle, and RT inhibitors can represent a promising pathway in treating AIDS.
Tao Zhang +8 more
doaj +2 more sources
Non-Nucleoside Reverse Transcriptase Inhibitors Join Forces with Integrase Inhibitors to Combat HIV [PDF]
Pharmaceuticals, 2020 In the treatment of acquired immune deficiency syndrome (AIDS), the diarylpyrimidine (DAPY) analogs etravirine (ETR) and rilpivirine (RPV) have been widely effective against human immunodeficiency virus (HIV) variants that are resistant to other non ...
Daniel M. Himmel, Eddy Arnold
doaj +2 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
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
Journal 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.
Christophe Pannecouque +2 more
exaly +7 more sources