Tri‐substituted 1,3,5‐triazine‐based analogs as effective HIV‐1 non‐nucleoside reverse transcriptase inhibitors (NNRTIs): A systematic review
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DOI: 10.1002/ddr.22154
Abstract: Non‐nucleoside reverse transcriptase inhibitors (NNRTIs) have significantly impacted the HIV‐1 wild‐type due to their high specificity and superior potency. As well as different combinations of NNRTIs have been used on clinically approved combining highly active… read more here.
Keywords: hiv; non nucleoside; drug; nucleoside reverse ... See more keywords
Fluoride Pharmacokinetics in Urine and Plasma Following Multiple Doses of MK-8507, an Investigational, Oral, Once-Weekly Non-Nucleoside Reverse Transcriptase Inhibitor.
Sign Up to like & getrecommendations! Published in 2021 at "Journal of clinical pharmacology"
DOI: 10.1002/jcph.1957
Abstract: MK-8507 is an investigational human immunodeficiency virus-1 (HIV-1) non-nucleoside reverse transcriptase inhibitor being developed for the treatment of HIV-1 infection. MK-8507 contains two trifluoromethyl groups that may result in fluoride release through metabolism, but the… read more here.
Keywords: non; nucleoside reverse; 8507 investigational; non nucleoside ... See more keywords
Deuteration Strategy-Inspired Design of Novel Diarylpyrimidine Derivatives as Potent Non-Nucleoside Reverse Transcriptase Inhibitors Featuring Improved Efficacy, Selectivity, and Druggability.
Sign Up to like & getrecommendations! Published in 2025 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.5c00202
Abstract: Deuteration strategy holds significant importance in the field of drug development. In this study, the deuteration strategy was applied to incorporate deuterated methyl groups at the metabolic sites where methyl groups were originally present, with… read more here.
Keywords: deuteration strategy; druggability; non nucleoside; deuteration ... See more keywords
Nucleoside reverse transcriptase inhibitors (NRTIs) induce proinflammatory cytokines in the CNS via Wnt5a signaling
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DOI: 10.1038/s41598-017-03446-w
Abstract: HAART is very effective in suppressing HIV-1 replication in patients. However, patients staying on long-term HAART still develop various HIV-associated neurological disorders, even when the viral load is low. The underlying pathogenic mechanisms are largely… read more here.
Keywords: wnt5a; proinflammatory cytokines; nucleoside reverse; wnt5a signaling ... See more keywords
Discovery of piperidine-substituted thiazolo[5,4-d]pyrimidine derivatives as potent and orally bioavailable HIV-1 non-nucleoside reverse transcriptase inhibitors
Sign Up to like & getrecommendations! Published in 2019 at "Communications Chemistry"
DOI: 10.1038/s42004-019-0174-8
Abstract: HIV-1 reverse transcriptase offers a key target for antiviral therapy. However, the rapid emergence of drug-resistant mutations in reverse transcriptase as well as the poor pharmacokinetic properties of HIV-1 non-nucleoside reverse transcriptase inhibitors (NNRTIs) limits… read more here.
Keywords: transcriptase inhibitors; nucleoside reverse; reverse; non nucleoside ... See more keywords
A Concise Analytical Profile of Efavirenz: Analytical Methodologies.
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DOI: 10.1080/10408347.2021.1895711
Abstract: Non-nucleoside reverse transcriptase inhibitors are the prime members of antiretroviral therapy that are presently employed for the management of the human immunodeficiency virus. It uses an enzyme i.e., reverse transcriptase to convert its ribonucleic acid… read more here.
Keywords: antiretroviral therapy; nucleoside reverse; reverse; non nucleoside ... See more keywords
The latest developments in the design and discovery of non-nucleoside reverse transcriptase inhibitors (NNRTIs) for the treatment of HIV
Sign Up to like & getrecommendations! Published in 2024 at "Expert Opinion on Drug Discovery"
DOI: 10.1080/17460441.2024.2415309
Abstract: ABSTRACT Introduction This review encapsulates the recent strides in the development of non-nucleoside reverse transcriptase inhibitors (NNRTIs) for HIV treatment, focusing on the novel structural designs that promise to overcome limitations of existing therapies, such… read more here.
Keywords: transcriptase inhibitors; non nucleoside; drug; nucleoside reverse ... See more keywords
Ritonavir-Boosted Darunavir Plus Two Nucleoside Reverse Transcriptase Inhibitors versus Other Regimens for Initial Antiretroviral Therapy for People with HIV Infection: A Systematic Review
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DOI: 10.1155/2017/2345617
Abstract: Background Darunavir is a second-generation protease-inhibitor used with ritonavir (DRV/r) and two nucleoside reverse-transcriptase inhibitors as an option in first-line antiretroviral treatment (ART). Methods We systematically reviewed randomized controlled trials (RCTs) of DRV/r versus other… read more here.
Keywords: transcriptase inhibitors; ritonavir boosted; nucleoside reverse; ritonavir ... See more keywords
Efficacy of second-line dolutegravir plus 2 nucleoside reverse transcriptase inhibitors by baseline nucleoside reverse transcriptase inhibitor resistance and nucleoside reverse transcriptase inhibitor use in the DAWNING study
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DOI: 10.1177/13596535221077487
Abstract: Background In the DAWNING study, dolutegravir + 2 nucleoside reverse transcriptase inhibitors (NRTIs) demonstrated superior efficacy at Week 48 and a favourable safety profile compared with lopinavir/ritonavir + 2 NRTIs in adults with HIV-1 failing… read more here.
Keywords: nucleoside reverse; reverse transcriptase; transcriptase inhibitor;
Multicenter study of skin rashes and hepatotoxicity in antiretroviral-naïve HIV-positive patients receiving non-nucleoside reverse-transcriptase inhibitor plus nucleoside reverse-transcriptase inhibitors in Taiwan
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DOI: 10.1371/journal.pone.0171596
Abstract: Objectives Two nucleos(t)ide reverse-transcriptase inhibitors (NRTIs) plus 1 non-NRTI (nNRTI) remain the preferred or alternative combination antiretroviral therapy (cART) for antiretroviral-naive HIV-positive patients in Taiwan. The three most commonly used nNRTIs are nevirapine (NVP), efavirenz… read more here.
Keywords: nucleoside reverse; hepatotoxicity; reverse transcriptase; hiv positive ... See more keywords
Development of novel S-N3-DABO derivatives as potent non-nucleoside reverse transcriptase inhibitors with improved potency and selectivity.
Sign Up to like & getrecommendations! Published in 2022 at "European journal of medicinal chemistry"
DOI: 10.2139/ssrn.4276520
Abstract: Following on our initial discovery of S-CN-DABOs as non-nucleoside reverse transcriptase inhibitors (NNRTIs), a series of novel S-N3-DABO derivatives F1-F31 were developed by substituting the cyano group of S-CN-DABOs with azide group. Some of these… read more here.
Keywords: potency; reverse transcriptase; reverse; nucleoside reverse ... See more keywords