Research Progress in HIV and Mycobacterium tuberculosis Inhibitors Containing Sulfonamide Moiety
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
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
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]
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
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 ...
Sheng Han +7 more
openalex +2 more sources
A novel series of uracil-bearing DAPYs derivatives were designed and synthesized via structure-based molecular hybridization to discover compounds with improved anti-resistance profiles. Anti-HIV activity of the designed compounds was tested in MT-4 cell
Heng Zhang +9 more
openalex +3 more sources
Optimization of the antiviral potency and lipophilicity of halogenated 2,6-diarylpyridinamines as a novel class of HIV-1 NNRTIS. [PDF]
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]
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
การศึกษาอันตรกิริยาของอนุพันธ์ควิโนลีนกับเอนไซม์ HIV-1 RT โดยใช้เทคนิคทางเคมีควอนตัม [PDF]
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
Synthesis, anti-HIV activity and molecular modeling study of some new pyrimidine analogues [PDF]
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
core +1 more source
Current state-of-the-art in preclinical and clinical development of novel non-nucleoside HIV-1 reverse transcriptase inhibitors [PDF]
In spite of the tremendous advance in our understanding of the HIV-1 life cycle and of the molecular mechanisms underlying its pathogenesis, it is still not possible to fully control the HIV-1 infection for long periods of time, not to mention eradicate ...
Giovanni Maga, SILVESTRI, Romano
core +1 more source

