Zobrazeno 1 - 10 of 48 pro vyhledávání: '"Graziella Tocco"'
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Akademický článek
Dihydroxyphenyl- and Heteroaromatic-Based Thienopyrimidinones to Tackle HIV-1 LEDGF/p75-Dependent IN Activity
Autor: Graziella Tocco, Serena Canton, Antonio Laus, Pierluigi Caboni, Stuart F. J. Le Grice, Enzo Tramontano, Francesca Esposito
Publikováno v: Molecules, Vol 28, Iss 18, p 6700 (2023)
The spread of Human Immunodeficiency Virus (HIV) still represents a global public health issue of major concern, and would benefit from unveiling unique viral features as targets for drug design. In this respect, HIV-1 integrase (IN), due to the abse
Externí odkaz: https://doaj.org/article/d47492d260c4445c9dbb6b7e0ebcdb24
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3
Akademický článek
Scaffold hopping and optimisation of 3’,4’-dihydroxyphenyl- containing thienopyrimidinones: synthesis of quinazolinone derivatives as novel allosteric inhibitors of HIV-1 reverse transcriptase-associated ribonuclease H
Autor: Graziella Tocco, Francesca Esposito, Pierluigi Caboni, Antonio Laus, John A. Beutler, Jennifer A. Wilson, Angela Corona, Stuart F. J. Le Grice, Enzo Tramontano
Publikováno v: Journal of Enzyme Inhibition and Medicinal Chemistry, Vol 35, Iss 1, Pp 1953-1963 (2020)
Bioisosteric replacement and scaffold hopping are powerful strategies in drug design useful for rationally modifying a hit compound towards novel lead therapeutic agents. Recently, we reported a series of thienopyrimidinones that compromise dynamics
Externí odkaz: https://doaj.org/article/40894ef0f11243f0834cdd5811c7e26e
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4
Akademický článek
U-47700 and Its Analogs: Non-Fentanyl Synthetic Opioids Impacting the Recreational Drug Market
Autor: Michael H. Baumann, Graziella Tocco, Donna M. Papsun, Amanda L. Mohr, Melissa F. Fogarty, Alex J. Krotulski
Publikováno v: Brain Sciences, Vol 10, Iss 11, p 895 (2020)
The recreational use of opioid drugs is a global threat to public health and safety. In particular, an epidemic of opioid overdose fatalities is being driven by illicitly manufactured fentanyl, while novel synthetic opioids (NSOs) are appearing on re
Externí odkaz: https://doaj.org/article/b3c9fc0e518c443ab2522a31706f09c5
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5
Akademický článek
Evaluation of Photoluminescence Properties of Some Poly(ethylene glycol) – Supported Coumarin Derivatives
Autor: Graziella Tocco, Carlo Maria Carbonaro, Gabriele Meli, Gianni Podda
Publikováno v: Molecules, Vol 14, Iss 3, Pp 1044-1055 (2009)
The immobilization of some coumarin derivatives on modified poly(ethylene glycol)s is reported and the influence of the polymeric support on the photoluminescence activity of the compounds is discussed. Upon ultraviolet excitation, the derivatives sh
Externí odkaz: https://doaj.org/article/9adce99d946748508d55c1ee040cfdbd
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6
Akademický článek
Solvent-Free Addition of Indole to Aldehydes: Unexpected Synthesis of Novel 1-[1-(1H-Indol-3-yl) Alkyl]-1H-Indoles and Preliminary Evaluation of Their Cytotoxicity in Hepatocarcinoma Cells
Autor: Graziella Tocco, Gloria Zedda, Mariano Casu, Gabriella Simbula, Michela Begala
Publikováno v: Molecules, Vol 22, Iss 10, p 1747 (2017)
New 1-[1-(1H-indol-3-yl) alkyl]-1H-indoles, surprisingly, have been obtained from the addition of indole to a variety of aldehydes under neat conditions. CaO, present in excess, was fundamental for carrying out the reaction with paraformaldehyde. Und
Externí odkaz: https://doaj.org/article/b21ae6c2a64c4260950cdfd4f0742ad7
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8
3-[3-(Phenalkylamino)cyclohexyl]phenols: Synthesis, biological activity, and in silico investigation of a naltrexone-derived novel class of MOR-antagonists
Autor: Graziella Tocco, Antonio Laus, Maksims Vanejevs, Anastasija Ture, Rafaela Mostallino, Nicholas Pintori, Maria Antonietta De Luca, M. Paola Castelli, Gaetano Di Chiara
Publikováno v: Archiv der PharmazieREFERENCES. 356(1)
The development of novel μ-opioid receptor (MOR) antagonists is one of the main objectives of drug discovery and development. Based on a simplified version of the morphinan scaffold, 3-[3-(phenalkylamino)cyclohexyl]phenol analogs were designed, synt
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f81d008490a160b7377e66c4c04a85dc
https://pubmed.ncbi.nlm.nih.gov/36328777
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9
Electron-Deficient Alkynes as Powerful Tools against Root-Knot Nematode Melodogyne incognita: Nematicidal Activity and Investigation on the Mode of Action
Autor: Pierluigi Caboni, Graziella Tocco, Nicola Sasanelli, Kodjo Eloh, Antonio Laus
Publikováno v: Journal of Agricultural and Food Chemistry
Journal of agricultural and food chemistry (Online) 68 (2020): 11088–11095. doi:10.1021/acs.jafc.0c00835
info:cnr-pdr/source/autori:Tocco G., Eloh K., Laus A., Sasanelli N., Caboni P./titolo:Electron deficient alkynes as powerful tools against root-knot nematode Meloidogyne incognita. Nemaaticidal activity and investigation on the mode of action./doi:10.1021%2Facs.jafc.0c00835/rivista:Journal of agricultural and food chemistry (Online)/anno:2020/pagina_da:11088/pagina_a:11095/intervallo_pagine:11088–11095/volume:68
The present study reports on the powerful nematicidal activity of a series of electron-deficient alkynes against the root-knot nematode Meloidogyne incognita (Kofoid and White) Chitwood. Interestingly, we found that the conjugation of electron-withdr
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c8b3e824b4db77f4bb79bb48ecf11636
https://doi.org/10.1021/acs.jafc.0c00835
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10
Scaffold hopping and optimisation of 3’,4’-dihydroxyphenyl- containing thienopyrimidinones: synthesis of quinazolinone derivatives as novel allosteric inhibitors of HIV-1 reverse transcriptase-associated ribonuclease H
Autor: Enzo Tramontano, Antonio Laus, Pierluigi Caboni, Angela Corona, Graziella Tocco, John A. Beutler, Stuart F. J. Le Grice, Jennifer A. Wilson, Francesca Esposito
Publikováno v: Journal of Enzyme Inhibition and Medicinal Chemistry, Vol 35, Iss 1, Pp 1953-1963 (2020)
Journal of Enzyme Inhibition and Medicinal Chemistry
article-version (VoR) Version of Record
Bioisosteric replacement and scaffold hopping are powerful strategies in drug design useful for rationally modifying a hit compound towards novel lead therapeutic agents. Recently, we reported a series of thienopyrimidinones that compromise dynamics
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a2e6e599d32f4b84af1e1eccbc1b3190
https://doaj.org/article/40894ef0f11243f0834cdd5811c7e26e
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