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
An integrated approach towards the discovery of novel non-nucleoside Leishmania major pteridine reductase 1 inhibitors.
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DOI: 10.1016/j.ejmech.2017.03.043
Abstract: Despite the fact that Leishmania ssp are pteridine auxotrophs, Dihydrofolate Reductase-Thymidylate Synthase (DHFR-TS) inhibitors are ineffective against Leishmania major. On the other hand Pteridine Reductase 1 (PTR1) inhibitors proved to be lethal to the parasite.… read more here.
Keywords: leishmania major; reductase; pteridine; non nucleoside ... See more keywords
Design, synthesis and primary biological evaluation of the novel 2-pyridone derivatives as potent non-nucleoside HBV inhibitors.
Sign Up to like & getrecommendations! Published in 2017 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2017.04.048
Abstract: In continuation of our efforts toward the discovery of potent non-nucleoside hepatitis B virus (HBV) inhibitors with novel structures, we have employed bioisosterism and hybrid pharmacophore-based strategy to explore the chemically diverse space of bioactive… read more here.
Keywords: hbv inhibitors; hbv; potent non; non nucleoside ... See more keywords
Novel natural non-nucleoside inhibitors of HIV-1 reverse transcriptase identified by shape- and structure-based virtual screening techniques.
Sign Up to like & getrecommendations! Published in 2019 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2018.10.029
Abstract: In this work we report a parallel application of both docking- and shape-based virtual screening (VS) methods, followed by Molecular Dynamics simulations (MDs), for discovering new compounds able to inhibit the human immunodeficiency virus type… read more here.
Keywords: virtual screening; based virtual; nucleoside inhibitors; non nucleoside ... See more keywords
Non-nucleoside reverse transcriptase inhibitor efavirenz activates PXR to induce hypercholesterolemia and hepatic steatosis.
Sign Up to like & getrecommendations! Published in 2019 at "Journal of hepatology"
DOI: 10.1016/j.jhep.2018.12.038
Abstract: BACKGROUND & AIMS The most prescribed non-nucleoside reverse transcriptase inhibitor, efavirenz, has been associated with elevated risk of dyslipidemia and hepatic steatosis in HIV-infected patients but the underlying mechanisms remain elusive. Herein, we investigated the… read more here.
Keywords: hepatic steatosis; efavirenz; non nucleoside; pxr ... See more keywords
Physiological Mg2+ Conditions Significantly Alter the Inhibition of HIV-1 and HIV-2 Reverse Transcriptases by Nucleoside and Non-Nucleoside Inhibitors in Vitro.
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DOI: 10.1021/acs.biochem.6b00943
Abstract: Reverse transcriptases (RTs) are typically assayed in vitro with 5-10 mM Mg2+, whereas the free Mg2+ concentration in cells is much lower. Artificially high Mg2+ concentrations used in vitro can misrepresent different properties of human… read more here.
Keywords: hiv; inhibition; non nucleoside; mg2 ... See more keywords
Structure-Aided Design, Synthesis, and Biological Evaluation of Potent and Selective Non-Nucleoside Inhibitors Targeting Protein Arginine Methyltransferase 5.
Sign Up to like & getrecommendations! Published in 2022 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.2c00398
Abstract: PRMT5 is a major type II protein arginine methyltransferase and plays important roles in diverse cellular processes. Overexpression of PRMT5 is implicated in various types of cancer. Many efforts have been made to develop potent… read more here.
Keywords: protein arginine; non nucleoside; arginine methyltransferase; potent selective ... 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
Etravirine and Rilpivirine Drug Resistance Among HIV-1 Subtype C Infected Children Failing Non-Nucleoside Reverse Transcriptase Inhibitor-Based Regimens in South India.
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DOI: 10.1089/aid.2016.0133
Abstract: We have analyzed reverse transcriptase (RT) region of HIV-1 pol gene from 97 HIV-infected children who were identified as failing first-line therapy that included first-generation non-nucleoside RT inhibitors (Nevirapine and Efavirenz) for at least 6… read more here.
Keywords: based regimens; non nucleoside; resistance; reverse transcriptase ... See more keywords
Development of novel S-N3-DABO derivatives as potent non-nucleoside reverse transcriptase inhibitors with improved potency and selectivity.
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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