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
An integrated approach towards the discovery of novel non-nucleoside Leishmania major pteridine reductase 1 inhibitors.
Sign Up to like & getrecommendations! Published in 2017 at "European journal of medicinal chemistry"
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.
Sign Up to like & getrecommendations! Published in 2017 at "Biochemistry"
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 gem-Dimethyl-hydroxymethylpyridine Derivatives as Potent Non-nucleoside RSV Polymerase Inhibitors.
Sign Up to like & getrecommendations! Published in 2024 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.4c00525
Abstract: Respiratory syncytial virus (RSV) is an RNA virus infecting the upper and lower respiratory tract and is recognized as a major respiratory health threat, particularly to older adults, immunocompromised individuals, and young children. Around 64… read more here.
Keywords: chemistry; non nucleoside; dimethyl hydroxymethylpyridine; hydroxymethylpyridine derivatives ... See more keywords
An Amazing 30-Year Journey around the DABO Family: A Medicinal Chemistry Lesson on a Versatile Class of Non-nucleoside HIV-1 Reverse Transcriptase Inhibitors
Sign Up to like & getrecommendations! Published in 2025 at "Journal of Medicinal Chemistry"
DOI: 10.1021/acs.jmedchem.4c02848
Abstract: Since the emergence of AIDS, the non-nucleoside HIV-1 RT inhibitors (NNRTIs) have attracted the attention of scientists and clinicians due to their high potency and specificity combined with low toxicity. 3,4-Dihydro-2-alkoxy-6-benzyl-4-oxopyrimidines (DABOs) are a family… read more here.
Keywords: chemistry; family; nucleoside hiv; 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