Zobrazeno 1 - 9
of 9
pro vyhledávání: '"Gianfranco Lopopolo"'
Autor:
Riccardo Ronchetti, Luigi Alfonso Pannone, Bruno Cerra, Emidio Camaioni, Gianfranco Lopopolo, Emanuele Attolino, Antimo Gioiello
Publikováno v:
Molecules, Vol 28, Iss 23, p 7859 (2023)
Mometasone furoate is a synthetic corticosteroid used in the treatment of skin inflammatory conditions, hay fever and asthma. The industrial manufacturing routes to mometasone furoate are generally accompanied by the formation of numerous process imp
Externí odkaz:
https://doaj.org/article/d976aa964adf42c7a81b6b6ca039c861
Publikováno v:
Crystals, Vol 13, Iss 8, p 1211 (2023)
Two solvates of estetrol have been isolated and characterized by SCXRD and PXRD as well as by thermal analyses, morphology and spectroscopy. Estetrol monohydrate (Estetrol.H2O, S.G. P1, Z = 12) contains 12 molecules in its asymmetric unit with very s
Externí odkaz:
https://doaj.org/article/d9860dea6fce4209b172f29210d48d14
Autor:
Flavio De Maio, Mariagrazia Rullo, Modesto de Candia, Rosa Purgatorio, Gianfranco Lopopolo, Giulia Santarelli, Valentina Palmieri, Massimiliano Papi, Gabriella Elia, Erica De Candia, Maurizio Sanguinetti, Cosimo Damiano Altomare
Publikováno v:
Viruses, Vol 14, Iss 8, p 1730 (2022)
Coagulation factor Xa (fXa) and thrombin (thr) are widely expressed in pulmonary tissues, where they may catalyze, together with the transmembrane serine protease 2 (TMPRSS2), the coronaviruses spike protein (SP) cleavage and activation, thus enhanci
Externí odkaz:
https://doaj.org/article/37a09714cf044919b8b60db65bfe2bb4
Autor:
Rosa Purgatorio, Nicola Gambacorta, Francesco Samarelli, Gianfranco Lopopolo, Modesto de Candia, Marco Catto, Orazio Nicolotti, Cosimo D. Altomare
Publikováno v:
Molecules, Vol 27, Iss 13, p 4269 (2022)
The rational discovery of new peptidomimetic inhibitors of the coagulation factor Xa (fXa) could help set more effective therapeutic options (to prevent atrial fibrillation). In this respect, we explored the conformational impact on the enzyme inhibi
Externí odkaz:
https://doaj.org/article/ce80e619bc244730a8c2370c8db82558
Autor:
Modesto de Candia, Cosimo Altomare, Gianfranco Lopopolo, Francesca Incampo, Mario Colucci, Giorgia Zaetta, Rocco Caliandro, Benny Danilo Belviso
Publikováno v:
Journal of medicinal chemistry 57 (2014): 8563–8575. doi:10.1021/jm5010754
info:cnr-pdr/source/autori:Belviso, Benny D.; Caliandro, Rocco; de Candia, Modesto; Zaetta, Giorgia; Lopopolo, Gianfranco; Incampo, Francesca; Colucci, Mario; Altomare, Cosimo D./titolo:How a beta-D-Glucoside Side Chain Enhances Binding Affinity to Thrombin of Inhibitors Bearing 2-Chlorothiophene as P1 Moiety: Crystallography, Fragment Deconstruction Study, and Evaluation of Antithrombotic Properties/doi:10.1021%2Fjm5010754/rivista:Journal of medicinal chemistry/anno:2014/pagina_da:8563/pagina_a:8575/intervallo_pagine:8563–8575/volume:57
info:cnr-pdr/source/autori:Belviso, Benny D.; Caliandro, Rocco; de Candia, Modesto; Zaetta, Giorgia; Lopopolo, Gianfranco; Incampo, Francesca; Colucci, Mario; Altomare, Cosimo D./titolo:How a beta-D-Glucoside Side Chain Enhances Binding Affinity to Thrombin of Inhibitors Bearing 2-Chlorothiophene as P1 Moiety: Crystallography, Fragment Deconstruction Study, and Evaluation of Antithrombotic Properties/doi:10.1021%2Fjm5010754/rivista:Journal of medicinal chemistry/anno:2014/pagina_da:8563/pagina_a:8575/intervallo_pagine:8563–8575/volume:57
The beta-d-glucose-containing compound 3, bearing 2-chlorothiophene and 1-isopropylpiperidine moieties as binders of the S1 and S4 pockets, respectively, proved to be potent competitive inhibitor of factor Xa (fXa, K-i = 0.090 nM) and thrombin (fIIa,
Autor:
Gianfranco Lopopolo, Luigi Panza, Modesto de Candia, Maria Rosaria Romano, Marcello D. Lograno, Francesco Campagna, Cosimo Altomare
Publikováno v:
ChemMedChem. 7:1669-1677
We synthesized a novel O-glucoside of the recently reported potent factor Xa (fXa) inhibitor 1, which bears a 5-chlorothien-2-yl moiety and 1-isopropylpiperidine as fragments that bind the S1 and S4 enzyme pockets, respectively. A β-D-glucosyl unit
Publikováno v:
Expert Opinion on Therapeutic Patents. 19:1535-1580
New oral anticoagulants with favorable safety profiles and fixed doses are required for the management of thromboembolism and stroke prevention in patients with atrial fibrillation. Among them, fXa inhibitors (the so-called xabans) are attractive opt
Autor:
Maria Rosaria Romano, Gianfranco Lopopolo, Filomena Fiorella, Modesto de Candia, Andrea Carotti, Marcello D. Lograno, Sophie Martel, Cosimo Altomare, Pierre-Alain Carrupt, Benny Danilo Belviso, Rocco Caliandro
Publikováno v:
Journal of medicinal chemistry 56 (2013): 8696–8711. doi:10.1021/jm401169a
info:cnr-pdr/source/autori:de Candia, Modesto; Fiorella, Filomena; Lopopolo, Gianfranco; Carotti, Andrea; Romano, Maria Rosaria; Lograno, Marcello Diego; Martel, Sophie; Carrupt, Pierre-Alain; Belviso, Benny D.; Caliandro, Rocco; Altomare, Cosimo/titolo:Synthesis and Biological Evaluation of Direct Thrombin Inhibitors Bearing 4-(Piperidin-1-yl)pyridine at the P1 Position with Potent Anticoagulant Activity/doi:10.1021%2Fjm401169a/rivista:Journal of medicinal chemistry/anno:2013/pagina_da:8696/pagina_a:8711/intervallo_pagine:8696–8711/volume:56
info:cnr-pdr/source/autori:de Candia, Modesto; Fiorella, Filomena; Lopopolo, Gianfranco; Carotti, Andrea; Romano, Maria Rosaria; Lograno, Marcello Diego; Martel, Sophie; Carrupt, Pierre-Alain; Belviso, Benny D.; Caliandro, Rocco; Altomare, Cosimo/titolo:Synthesis and Biological Evaluation of Direct Thrombin Inhibitors Bearing 4-(Piperidin-1-yl)pyridine at the P1 Position with Potent Anticoagulant Activity/doi:10.1021%2Fjm401169a/rivista:Journal of medicinal chemistry/anno:2013/pagina_da:8696/pagina_a:8711/intervallo_pagine:8696–8711/volume:56
The design and synthesis of a new class of nonpeptide direct thrombin inhibitors, built on the structure of 1-(pyridin-4-yl)piperidine-4-carboxamide, are described. Starting from a strongly basic 1-amidinopiperidine derivative (6) showing poor thromb
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6737437b86d975ef8a8c7f9e21f5b5de
http://www.cnr.it/prodotto/i/305511
http://www.cnr.it/prodotto/i/305511
Autor:
Filomena Fiorella, Pierre-Alain Carrupt, Gianfranco Lopopolo, Cosimo Altomare, Sophie Martel, Orazio Nicolotti, Modesto de Candia
Publikováno v:
European Journal of Pharmaceutical Sciences, Vol. 42 (2011) pp. 180-190
New chloro-substituted biarylmethoxyphenyl piperidine-4-carboxamides were synthesized and assayed in vitro as inhibitors of the blood coagulation enzymes factor Xa (fXa) and thrombin. An investigation of effects of the amidine and isopropyl groups at