Results 11 to 20 of about 148 (100)

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

Further Exploring Solvent-Exposed Tolerant Regions of Allosteric Binding Pocket for Novel HIV-1 NNRTIs Discovery. [PDF]

ACS Med Chem Lett, 2018
Based on the detailed analysis of the binding mode of diarylpyrimidines (DAPYs) with HIV-1 RT, we designed several subseries of novel NNRTIs, with the aim to probe biologically relevant chemical space of solvent-exposed tolerant regions in NNRTIs binding
Kang D, Wang Z, Zhang H, Wu G, Zhao T, Zhou Z, Huo Z, Huang B, Feng D, Ding X, Zhang J, Zuo X, Jing L, Luo W, Guma S, Daelemans D, Clercq E, Pannecouque C, Zhan P, Liu X.   +19 more
europepmc   +3 more sources

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, Vijay Kumar Siripuram   +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, Kerri J. Penrose, Amy L. Heaps, Elias K. Halvas, B. Jay Goetz, Kelley C. Gordon, Russell Hardesty, Rahil Sethi, William Schwarzmann, Daniel W. Szydlo, Marla J. Husnik, Uma Chandran, Thesla Palanee‐Phillips, Jared M. Baeten, John W. Mellors, the MTN‐020 Study Team   +15 more
wiley   +1 more source

Structure-Based Discovery of Novel NH₂‑Biphenyl-Diarylpyrimidines as Potent Non-Nucleoside Reverse Transcriptase Inhibitors with Significantly Improved Safety: From NH₂‑Naphthyl-Diarylpyrimidine to NH₂‑Biphenyl-Diarylpyrimidine

, 2022
Results from recently completed studies suggested that the NH2-naphthyl-diarylpyrimidine JX-7 displayed remarkable inhibitory activity against wild-type HIV-1 (EC50 = 5 nM) and numerous clinically observed variants in MT-4 cells; however, its high ...
Fen-Er Chen (2495434), Erik De Clercq (7541327), Xin Jin (108988), Christophe Pannecouque (496139), Wen-Juan Huang (394683), Li-Min Zhao (10748487), Shuai Wang (109515), Yin-Xiang Zhang (12710306)   +7 more
core   +3 more sources

The Need for Development of New HIV‐1 Reverse Transcriptase and Integrase Inhibitors in the Aftermath of Antiviral Drug Resistance

Scientifica, Volume 2012, Issue 1, 2012., 2012
The use of highly active antiretroviral therapy (HAART) involves combinations of drugs to achieve maximal virological response and reduce the potential for the emergence of antiviral resistance. There are two broad classes of reverse transcriptase inhibitors, the nucleoside reverse transcriptase inhibitors (NRTIs) and nonnucleoside reverse ...
Mark A. Wainberg, Massimo Clementi, Christophe Marchand, Hans J. Netter, Blake Peterson   +4 more
wiley   +1 more source

Exploiting the Tolerant Region I of the Non-Nucleoside Reverse Transcriptase Inhibitor (NNRTI) Binding Pocket: Discovery of Potent Diarylpyrimidine-Typed HIV‑1 NNRTIs against Wild-Type and E138K Mutant Virus with Significantly Improved Water Solubility and Favorable Safety Profiles

, 2019
Diarylpyrimidine derivatives (DAPYs) exhibit robust anti-HIV-1 potency, although they have been compromised by E138K variant and severe side-effects and been suffering from poor water solubility.
Dongwei Kang (3080175), Peng Zhan (433925), Erik De Clercq (55639), Ping Gao (172038), Wenmin Chen (6378056), Jian Zhang (1682), Dirk Daelemans (397676), Xinyong Liu (1730737), Tong Zhao (17215), Boshi Huang (3080169), Francisco Javier Luque (2519383), Zhenyu Li (295387), Christophe Pannecouque (496139), Xiangyi Jiang (6378059), Ye Tian (220278), Tiziana Ginex (3662398), David Vílchez (6378062)   +16 more
core   +2 more sources

A Review on Medicinal Chemistry and Biological Activity of Dihydropyrimidinones Against HIV

Archiv der Pharmazie, Volume 359, Issue 4, April 2026.
This article presents the latest advances in the development of dihydropyrimidinone (DHPM) derivatives as promising candidates against HIV. By exploring their interactions with essential viral targets and highlighting innovative compounds with potent antiviral activity, we provide an updated perspective on the opportunities for new antiretroviral ...
Debora I. Leite, Fernando B. Macedo, Murilo Marinho de C. Lima, Isabelle S. Brum, Jonathan Fragoso Miranda de Oliveira, Ana Clara S. Costa, Stella C. Duarte, Sarah Moon, Stefany de Castro B. Moura, Andressa P. de Oliveira, Nubia Boechat, Monica M. Bastos   +11 more
wiley   +1 more source

A series of diaryltriazines and diarylpyrimidines are highly potent nonnucleoside reverse transcriptase inhibitors with possible applications as microbicides. [PDF]

Antimicrob Agents Chemother, 2004
An in vitro model of monocyte-derived dendritic cells (MO-DC) and CD4(+) T cells, representing the primary targets of sexual human immunodeficiency virus (HIV) transmission, was used to evaluate the antiviral and immune suppressive activity of new ...
Van Herrewege Y, Vanham G, Michiels J, Fransen K, Kestens L, Andries K, Janssen P, Lewi P.   +7 more
europepmc   +2 more sources

Incorporating Heavy Atom Effect onto Molecular Rotors for Realizing Exceptionally Photocatalytic Oxidation Reaction under Low‐Temperature Conditions

Advanced Materials Interfaces, Volume 13, Issue 3, 3 February 2026.
Here, we reported a series of molecular‐rotor‐based photoactivated oxidase mimics, DAPy‐Xm, in which heavy atom incorporation enhances both ROS generation and cold‐adapted property. Among them, DAPy‐Im enables efficient photo‐oxidation of ergosterol and photocatalytic H2O2 production at low temperature.
Barbara Zenabu Anibea, Wen‐Chu Wu, Ching‐Ping Liu, Wei‐Min Liu   +3 more
wiley   +1 more source