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Monica Demurtas  - - - 
Top co-authors
Valentina Onnis

141 shared publications

A Department of Life and Environmental Sciences - Unit of Pharmaceutical, Pharmacological and Nutraceutical Sciences , University of Cagliari , Cagliari , Italy

Jan Balzarini

78 shared publications

KU Leuven—University of Leuven, Department of Microbiology and Immunology, Rega Institute for Medical Research, Laboratory of Virology and Chemotherapy, Leuven B-3000, Belgium;(S.L.);(J.B.)

Sandra Liekens

33 shared publications

KU Leuven—University of Leuven, Department of Microbiology and Immunology, Rega Institute for Medical Research, Laboratory of Virology and Chemotherapy, Leuven B-3000, Belgium;(S.L.);(J.B.)

Salvatore Pacifico

26 shared publications

Department of Chemical and Pharmaceutical Sciences, University of Ferrara, 44121 Ferrara, Italy

Alessandro Deplano

24 shared publications

Department of Life and Environmental Sciences – Unit of Pharmaceutical, Pharmacological and Nutraceutical Sciences, University of Cagliari, Cagliari, Italy

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Publication Record
Distribution of Articles published per year 
(2015 - 2018)
Total number of journals
published in
 
5
 
Publications See all
Article 0 Reads 1 Citation Benzofuran hydrazones as potential scaffold in the development of multifunctional drugs: Synthesis and evaluation of ant... Anna Baldisserotto, Monica Demurtas, Ilaria Lampronti, David... Published: 01 August 2018
European Journal of Medicinal Chemistry, doi: 10.1016/j.ejmech.2018.07.001
DOI See at publisher website
Article 0 Reads 3 Citations Novel propanamides as fatty acid amide hydrolase inhibitors Alessandro Deplano, Carmine Marco Morgillo, Monica Demurtas,... Published: 01 August 2017
European Journal of Medicinal Chemistry, doi: 10.1016/j.ejmech.2017.05.033
DOI See at publisher website PubMed View at PubMed
Article 0 Reads 3 Citations Design, synthesis and antiviral evaluation of novel heteroarylcarbothioamide derivatives as dual inhibitors of HIV-1 rev... Angela Corona, Valentina Onnis, Alessandro Deplano, Giulia B... Published: 10 July 2017
Pathogens and Disease, doi: 10.1093/femspd/ftx078
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In the continuous effort to identify new HIV-1 inhibitors endowed with innovative mechanisms, the dual inhibition of different viral functions would provide a significant advantage against drug-resistant variants. The HIV-1 reverse transcriptase (RT)-associated ribonuclease H (RNase H) is the only viral-encoded enzymatic activity that still lacks an efficient inhibitor. We synthesized a library of 3,5-diamino-N-aryl-1H-pyrazole-4-carbothioamide and 4-amino-5-benzoyl-N-phenyl-2-(substituted-amino)-1H-pyrrole-3-carbothioamide derivatives and tested them against RNase H activity. We identified the pyrazolecarbothioamide derivative A15, able to inhibit viral replication and both RNase H and RNA-dependent DNA polymerase (RDDP) RT-associated activities in the low micromolar range. Docking simulations hypothesized its binding to two RT pockets. Site-directed mutagenesis experiments showed that, with respect to wt RT, V108A substitution strongly reduced A15 IC50 values (12.6-fold for RNase H inhibition and 4.7-fold for RDDP), while substitution A502F caused a 9.0-fold increase in its IC50 value for RNase H, not affecting the RDDP inhibition, reinforcing the hypothesis of a dual-site inhibition. Moreover, A15 retained good inhibition potency against three non-nucleoside RT inhibitor (NNRTI)-resistant enzymes, confirming a mode of action unrelated to NNRTIs and suggesting its potential as a lead compound for development of new HIV-1 RT dual inhibitors active against drug-resistant viruses.
Article 0 Reads 2 Citations Potent Nematicidal Activity of Maleimide Derivatives on Meloidogyne incognita Kodjo Eloh, Monica Demurtas, Manuel Giacomo Mura, Alessandro... Published: 09 June 2016
Journal of Agricultural and Food Chemistry, doi: 10.1021/acs.jafc.6b02250
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Article 5 Reads 4 Citations Design, Synthesis and Evaluation of Antiproliferative Activity of New Benzimidazolehydrazones Valentina Onnis, Monica Demurtas, Alessandro Deplano, Gianfr... Published: 30 April 2016
Molecules, doi: 10.3390/molecules21050579
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The synthesis and antiproliferative activity of new benzimidazole derivatives bearing an hydrazone mojety at the 2-position is described. The new N′-(4-arylidene)-1H-benzo[d]imidazole-2-carbohydrazides were evaluated for their cytostatic activity toward the murine leukemia (L1210), human T-cell leukemia (CEM), human cervix carcinoma (HeLa) and human pancreas carcinoma cells (Mia Paca-2). A preliminary structure-activity relationship could be defined. Some of the compounds possess encouraging and consistent antiproliferative activity, having IC50 values in the low micromolar range.
Article 0 Reads 3 Citations In Vitro Nematicidal Activity of Aryl Hydrazones and Comparative GC-MS Metabolomics Analysis Kodjo Eloh, Monica Demurtas, Alessandro Deplano, Alvine Ngou... Published: 10 November 2015
Journal of Agricultural and Food Chemistry, doi: 10.1021/acs.jafc.5b04815
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