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)
Ting-Ting Li +4 more
doaj +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
Bioisosterism-driven design of orally active, safe, and broad-spectrum biphenyl-DAPY derivatives as highly potent HIV-1 non-nucleoside reverse transcriptase inhibitors. [PDF]
Acta Pharm Sin BChen XM +5 more
europepmc +2 more sources
Improving Druggability of Novel Diarylpyrimidine NNRTIs by a Fragment-Based Replacement Strategy: From Biphenyl-DAPYs to Heteroaromatic-Biphenyl-DAPYs [PDF]
, 2021 Li Ding +4 more
openalex +3 more sources
Strategies in the Design and Development of Non-Nucleoside Reverse Transcriptase Inhibitors (NNRTIs). [PDF]
Viruses, 2023 Vanangamudi M +3 more
europepmc +1 more source