Cargando…

DB-02, a C-6-Cyclohexylmethyl Substituted Pyrimidinone HIV-1 Reverse Transcriptase Inhibitor with Nanomolar Activity, Displays an Improved Sensitivity against K103N or Y181C Than S-DABOs

6-(cyclohexylmethyl)-5-ethyl-2-((2-oxo-2-phenylethyl)thio)pyrimidin-4(3H)-one (DB-02) is a member of the newly reported synthetic anti-HIV-1 compounds dihydro-aryl/alkylsulfanyl-cyclohexylmethyl-oxopyrimidines, S-DACOs. In vitro anti-HIV-1 activity and resistance profile studies have suggested that...

Descripción completa

Detalles Bibliográficos
Autores principales:	Zhang, Xing-Jie, Lu, Li-He, Wang, Rui-Rui, Wang, Yue-Ping, Luo, Rong-Hua, Cong Lai, Christopher, Yang, Liu-Meng, He, Yan-Ping, Zheng, Yong-Tang
Formato:	Online Artículo Texto
Lenguaje:	English
Publicado:	Public Library of Science 2013
Materias:	Research Article
Acceso en línea:	https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3839930/ https://www.ncbi.nlm.nih.gov/pubmed/24282600 http://dx.doi.org/10.1371/journal.pone.0081489

Ejemplares similares

Mechanistic Study of Common Non-Nucleoside Reverse Transcriptase Inhibitor-Resistant Mutations with K103N and Y181C Substitutions
por: Lai, Ming-Tain, et al.
Publicado: (2016)

Scaffold Hopping in Discovery of HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitors: From CH(CN)-DABOs to CH(CN)-DAPYs
por: Li, Ting-Ting, et al.
Publicado: (2020)

Biophysical Characterization of Novel DNA Aptamers against K103N/Y181C Double Mutant HIV-1 Reverse Transcriptase
por: Ratanabunyong, Siriluk, et al.
Publicado: (2022)

Residue-Ligand Interaction Energy (ReLIE) on a Receptor-Dependent 3D-QSAR Analysis of S- and NH-DABOs as Non-Nucleoside Reverse Transcriptase Inhibitors
por: de Brito, Monique Araújo, et al.
Publicado: (2012)

6-Cyclohexylmethyl-2-cyclohexylsulfanyl-5-isopropylpyrimidin-4(3H)-one
por: Zhang, Chun-Sheng, et al.
Publicado: (2008)

N-(4-Bromophenyl)-2-[(1-cyclohexylmethyl-1H-1,2,4-triazol-3-yl)sulfanyl]acetamide
por: Wang, Yue-Ping, et al.
Publicado: (2012)

Cyclohexylmethyl Flavonoids Suppress Propagation of Breast Cancer Stem Cells via Downregulation of NANOG
por: Liao, Wen-Ying, et al.
Publicado: (2013)

6-Cyclohexylmethyl-5-ethyl-2-[(2-oxo-2-phenylethyl)sulfanyl]pyrimidin-4(3H)-one
por: Yan, Wan-Lu, et al.
Publicado: (2011)

Review of Oxepine-Pyrimidinone-Ketopiperazine Type Nonribosomal Peptides
por: Guo, Yaojie, et al.
Publicado: (2020)

1-Cyclohexylmethyl-3-methyl-2-[(phenylimino)(sulfido)methyl]benzimidazolium
por: Akkurt, Mehmet, et al.
Publicado: (2008)

RNA-Seq Reveals Protective Mechanisms of Mongolian Medicine Molor-Dabos-4 on Acute Indomethacin-Induced Gastric Ulcers in Rats
por: Bao, Terigele, et al.
Publicado: (2022)

Site-specific antitumour effects of 2 pyrimidinone compounds in rats.
por: Eggermont, A. M., et al.
Publicado: (1986)

Novel Trifluoromethyl Pyrimidinone Compounds With Activity Against Mycobacterium tuberculosis
por: Hembre, Erik, et al.
Publicado: (2021)

Discovery of the Novel Entecavir‐Resistant Hepatitis B Virus Reverse Transcriptase A181C Substitution From an Integrated Genotypic Analysis
por: Rose, Ronald E., et al.
Publicado: (2018)

The development of drug resistance mutations K103N Y181C and G190A in long term Nevirapine-containing antiviral therapy
por: Wang, Yuncong, et al.
Publicado: (2014)

Synthesis and Biological Evaluation of Benzo [4,5]- and Naphtho[2′,1′:4,5]imidazo[1,2-c]pyrimidinone Derivatives
por: Kamzeeva, Polina, et al.
Publicado: (2023)

Iron Oxide Nanoparticles with Supramolecular Ureido-Pyrimidinone Coating for Antimicrobial Peptide Delivery
por: Turrina, Chiara, et al.
Publicado: (2023)

MicroRNA-181c provides neuroprotection in an intracerebral hemorrhage model
por: Lu, Xi, et al.
Publicado: (2020)

Continuous-flow retro-Diels–Alder reaction: an efficient method for the preparation of pyrimidinone derivatives
por: Nekkaa, Imane, et al.
Publicado: (2018)

Impact of Y181C and/or H221Y mutation patterns of HIV-1 reverse transcriptase on phenotypic resistance to available non-nucleoside and nucleoside inhibitors in China
por: Guo, Wei, et al.
Publicado: (2014)

MicroRNA-181c Exacerbates Brain Injury in Acute Ischemic Stroke
por: Ma, Qingfeng, et al.
Publicado: (2016)

Modified DNA Aptamers for C-Reactive Protein and Lactate Dehydrogenase-5 with Sub-Nanomolar Affinities
por: Minagawa, Hirotaka, et al.
Publicado: (2020)

Synthesis and biological evaluation of a series of 2-(((5-akly/aryl-1H-pyrazol-3-yl)methyl)thio)-5-alkyl-6-(cyclohexylmethyl)-pyrimidin-4(3H)-ones as potential HIV-1 inhibitors
por: Wu, Yumeng, et al.
Publicado: (2020)

Green Synthesis and Urease Inhibitory Activity of Spiro-Pyrimidinethiones/Spiro-Pyrimidinones-Barbituric Acid Derivatives
por: Mohammadi Ziarani, Ghodsi, et al.
Publicado: (2015)

Regio- and stereoselective synthesis of benzothiazolo-pyrimidinones via an NHC-catalyzed Mannich/lactamization domino reaction
por: Ni, Qijian, et al.
Publicado: (2015)

Structure-based design, synthesis, and biological evaluation of novel pyrimidinone derivatives as PDE9 inhibitors
por: Wu, Xu-Nian, et al.
Publicado: (2018)

Synthesis of Novel 3H-Quinazolin-4-ones Containing Pyrazolinone, Pyrazole and Pyrimidinone Moieties
por: Saleh, Mohamed A., et al.
Publicado: (2003)

Molecular Docking and Biophysical Studies for Antiproliferative Assessment of Synthetic Pyrazolo-Pyrimidinones Tethered with Hydrazide-Hydrazones
por: Horchani, Mabrouk, et al.
Publicado: (2021)

Experimental and computational chemical studies on the corrosion inhibition of new pyrimidinone derivatives for copper in nitric acid
por: Fouda, A. S., et al.
Publicado: (2022)

Chemical Modification of Curcumin into Its Semi-Synthetic Analogs Bearing Pyrimidinone Moiety as Anticancer Agents
por: Afzal, Obaid, et al.
Publicado: (2022)

Discovery of Nanomolar-Affinity Pharmacological Chaperones Stabilizing the Oncogenic p53 Mutant Y220C
por: Stephenson Clarke, Joseph R., et al.
Publicado: (2022)

miR-103-3p Regulates the Proliferation and Differentiation of C2C12 Myoblasts by Targeting BTG2
por: He, Yulin, et al.
Publicado: (2023)

Synthesis and molecular modelling studies of pyrimidinones and pyrrolo[3,4-d]-pyrimidinodiones as new antiplasmodial compounds
por: Rogerio, Kamilla Rodrigues, et al.
Publicado: (2018)

New Pyrimidinone-Fused 1,4-Naphthoquinone Derivatives Inhibit the Growth of Drug Resistant Oral Bacteria
por: Kim, Kyungmin, et al.
Publicado: (2020)

Enhancing the Anticancer Potential of Targeting Tumor-Associated Metalloenzymes via VEGFR Inhibition by New Triazolo[4,3-a]pyrimidinone Acyclo C-Nucleosides Multitarget Agents
por: Abd Al Moaty, Mohamed Nabil, et al.
Publicado: (2022)

Phenotypic Test of Benzo[4,5]imidazo[1,2-c]pyrimidinone-Based Nucleoside and Non-Nucleoside Derivatives against DNA and RNA Viruses, Including Coronaviruses
por: Kamzeeva, Polina, et al.
Publicado: (2023)

MimoDB: a New Repository for Mimotope Data Derived from Phage Display Technology
por: Ru, Beibei, et al.
Publicado: (2010)

Cytotoxic T cell recognition of an HIV-1 reverse transcriptase variant peptide incorporating the K103N drug resistance mutation
por: Mahnke, Lisa, et al.
Publicado: (2006)

Sub-Nanomolar Sensitivity of Nitric Oxide Mediated Regulation of cGMP and Vasomotor Reactivity in Vascular Smooth Muscle
por: Held, Kara F., et al.
Publicado: (2012)

Nanomolar Inhibitors of Trypanosoma brucei RNA Triphosphatase
por: Smith, Paul, et al.
Publicado: (2016)

Cannot write session to /tmp/vufind_sessions/sess_07uasnneaibv6djg67j1qneacn