, 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
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
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
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Structural Studies and Structure Activity Relationships for Novel Computationally Designed Non-nucleoside Inhibitors and Their Interactions With HIV-1 Reverse Transcriptase [PDF]
, 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 ...
Anderson, Karen S. +7 more
core +1 more source
Research Progress in HIV and Mycobacterium tuberculosis Inhibitors Containing Sulfonamide Moiety
Journal of Chemistry, Volume 2023, Issue 1, 2023., 2023 Numerous studies have reported significant results regarding the efficacy of sulfonamides against Mycobacterium tuberculosis and various HIV strains. This scientific paper provides an overview of the progress made over a decade of sulfonamides against HIV‐1 and mycobacteria and its development against extremely drug‐resistant (XDR) and multidrug ...
Christiana Abimbola Salubi +1 more
wiley +1 more source
HIV‐1 drug resistance among individuals who seroconverted in the ASPIRE dapivirine ring trial
Journal of the International AIDS Society, Volume 24, Issue 11, November 2021., 2021 Abstract Introduction A potential concern with the use of dapivirine (DPV) for HIV prevention is the selection of a drug‐resistant virus that could spread and reduce the effectiveness of non‐nucleoside reverse transcriptase (NNRTI)‐based first‐line antiretroviral therapy.
Urvi M. Parikh +15 more
wiley +1 more source
Focus on chirality of HIV-1 non-nucleoside reverse transcriptase inhibitors [PDF]
, 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, Valeria, Silvestri, Romano
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การศึกษาอันตรกิริยาของอนุพันธ์ควิโนลีนกับเอนไซม์ HIV-1 RT โดยใช้เทคนิคทางเคมีควอนตัม [PDF]
, 2021 MASTER OF SCIENCE (M.Sc.)วิทยาศาสตรมหาบัณฑิต (วท.ม.)HIV-1 (Human Immunodeficiency Virus Type 1) is a major cause of AIDS and there are currently several inhibitors used to treat AIDS patients.
core
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
Synthesis, anti-HIV activity and molecular modeling study of some new pyrimidine analogues [PDF]
, 2014 A new series of 2,6-diamino-5-arylazo-4-chloropyrimidine analogues (6-13) were synthesized from the pyrimidine scaffold 5, via diazotization with various amines. Nucleophilic displacement of compound 5 by ethanethiolate or arylthio nucleophiles, afforded
Al-Masoudi +9 more
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