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16 results on '"Monica Donghi"'

1. Synthesis and evaluation of novel phosphoramidate prodrugs of 2′-methyl cytidine as inhibitors of hepatitis c virus NS5B polymerase

Author

Claudio Giuliano, Michael Rowley, Annalise Di Marco, Fabrizio Fiore, Monica Donghi, Cristina Gardelli, Barbara Attenni, Vincenzo Pucci, Frank Narjes, Ralph Laufer, and Joseph F. Leone

Subjects
Hepatitis C virus, Clinical Biochemistry, Drug Evaluation, Preclinical, Pharmaceutical Science, Cytidine, Hepacivirus, Viral Nonstructural Proteins, medicine.disease_cause, Biochemistry, chemistry.chemical_compound, Dogs, In vivo, Drug Discovery, medicine, Animals, Humans, Phosphoric Acids, Prodrugs, Nucleotide, Molecular Biology, Cells, Cultured, chemistry.chemical_classification, Organic Chemistry, Biological activity, Phosphoramidate, Prodrug, RNA-Dependent RNA Polymerase, Amides, In vitro, Rats, chemistry, Hepatocytes, Molecular Medicine, Rabbits
Abstract

A variety of new prodrugs of 2'-methyl cytidine based on acyloxy ethylamino phosphoramidates have been synthesized and tested in vitro and in vivo for their biological activity. Compared with the parent drug a 10- to 20-fold increase in formation of nucleotide triphosphate in rat and human hepatocytes could be achieved.

Published
2009

2. Patent Strategy in Pharmaceutical Industry: Are Additional Patents Valuable?

Author

Monica Donghi and Monica Donghi

Subjects
Drugs--Patents--Economic aspects--European U, Patent medicines--Law and legislation--Europea, Patent medicines--European Union countries--Ca
Abstract

Dieses Buch untersucht die Lifecycle-Management-Strategien, die von Pharma-Unternehmen eingesetzt werden, um den Wert ihres Produktportfolios zu maximieren. Solche Strategien werden manchmal von Generika-Unternehmen als „evergreening“ bezeichnet. Die Analyse erfolgt anhand zwei zufällig ausgewählter „Blockbuster“-Medikamente, Taxotere und Xalatan und konzentriert sich auf zwei dieser Strategien, nämlich die Produktverbesserung und die Produktlinienerweiterung.In englischer Sprache.

Published
2014

5. Taxol Semisynthesis: A Highly Enantio- and Diastereoselective Synthesis of the Side Chain and a New Method for Ester Formation at C-13 Using Thioesters

Author

Anna Vulpetti, Ermes Vanotti, Nicola Mongelli, Monica Donghi, Cesare Gennari, and Michela Carcano

Subjects
chemistry.chemical_compound, Addition reaction, chemistry, Docetaxel, Paclitaxel, Stereochemistry, Organic Chemistry, Imine, medicine, Side chain, Combinatorial chemistry, Semisynthesis, medicine.drug
Abstract

A very simple, new, and straightforward approach to the Paclitaxel (Taxol) and Docetaxel (Taxotere) side chains has been developed using the imine addition reaction of thioester-derived boron enola...

Published
1997

7. ChemInform Abstract: Taxol Semisynthesis: A Highly Enantio- and Diastereoselective Synthesis of the Side Chain and a New Method for Ester Formation at C- 13 Using Thioesters

Author

Anna Vulpetti, Ermes Vanotti, Monica Donghi, Cesare Gennari, Nicola Mongelli, and Michela Carcano

Subjects
Addition reaction, Imine, chemistry.chemical_element, General Medicine, Combinatorial chemistry, Semisynthesis, Terpene, chemistry.chemical_compound, Docetaxel, chemistry, Paclitaxel, medicine, Side chain, Boron, medicine.drug
Abstract

A very simple, new, and straightforward approach to the Paclitaxel (Taxol) and Docetaxel (Taxotere) side chains has been developed using the imine addition reaction of thioester-derived boron enola...

Published
2010

9. ChemInform Abstract: Synthesis of a Hexahydropyrimido[1,2-a]azepine-2-carboxamide Derivative (I) Useful as an HIV Integrase Inhibitor

Author

Cristina Gardelli, Silvia Pesci, Vincenzo Summa, Marco Ferrara, Monica Donghi, Benedetta Crescenzi, Emanuela Nizi, and Ester Muraglia

Subjects
Anti hiv activity, biology, medicine.drug_class, Stereochemistry, Carboxamide, General Medicine, Combinatorial chemistry, Integrase, chemistry.chemical_compound, chemistry, medicine, biology.protein, Azepine, Derivative (chemistry)
Published
2008

11. Structure-based design of amidinophenylurea-derivatives for factor VIIa inhibition

Author

Martin Lorenz, Hans Peter Nestler, Otmar Klingler, Monica Donghi, Manfred Schudok, Herman Schreuder, Hauke Szillat, Joerg Czech, and Hans Matter

Subjects
Molecular model, Stereochemistry, Clinical Biochemistry, Pharmaceutical Science, Factor VIIa, Crystallography, X-Ray, Biochemistry, Chemical synthesis, Fibrinolytic Agents, Drug Discovery, Binding site, Molecular Biology, Serine protease, Binding Sites, biology, Molecular Structure, Chemistry, Protease binding, Phenylurea Compounds, Organic Chemistry, Docking (molecular), Enzyme inhibitor, Drug Design, biology.protein, Molecular Medicine, Fibrinolytic agent, Peptide Hydrolases
Abstract

The amidinophenylurea scaffold was earlier shown to provide an excellent template for the synthesis of novel and potent inhibitors of the blood coagulation factor VIIa. In this contribution we describe the structure-based design of potent ligands guided by X-ray crystallography, molecular modeling and docking studies. The design and synthetic efforts were directed towards novel modifications to explore the protease binding region close to the S4 subsite.

Published
2004

13. Discovery of Raltegravir, a Potent, Selective Orally Bioavailable HIV-Integrase Inhibitor for the Treatment of HIV-AIDS Infection.

Author

Vincenzo Summa, Alessia Petrocchi, Fabio Bonelli, Benedetta Crescenzi, Monica Donghi, Marco Ferrara, Fabrizio Fiore, Cristina Gardelli, Odalys Gonzalez Paz, Daria J. Hazuda, Philip Jones, Olaf Kinzel, Ralph Laufer, Edith Monteagudo, Ester Muraglia, Emanuela Nizi, Federica Orvieto, Paola Pace, Giovanna Pescatore, and Rita Scarpelli

Published
2008
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16. Stereocontrolled synthesis of polyketide libraries: Boron-mediated aldol reactions with aldehydes on solid support

Author

Umberto Piarulli, Cesare Gennari, Simona Ceccarelli, Ian Paterson, Karim Aboutayab, and Monica Donghi

Subjects
Silylation, Stereochemistry, Chemistry, Organic Chemistry, Enantioselective synthesis, chemistry.chemical_element, Biochemistry, Adduct, Polyketide, Aldol reaction, Drug Discovery, Aldol condensation, Boron, Linker
Abstract

Two complementary classes of chiral boron enolates for adaptation to aldol additions to resin-bound aldehydes were studied: (i) the thioester-derived enolate 1 bearing chiral ligands on boron, and (ii) the chiral ketone-derived enolate 2. The viability of performing highly enantioselective, boron-mediated, aldol reactions was demonstrated by the preparation of resin-bound adducts 15 (91% ee) and 21 (88% ee). The solid phase aldol reactions of enolate 2 can be combined with an in situ reduction of the intermediate aldolate using LiBH4, leading to the controlled introduction of four contiguous stereocentres, as in 33→40 (>96% diastereoselectivity). The choice of linker is crucial and the available experimental evidence suggests that trityl and silyl linkers are optimal. This methodology should be amenable to the stereocontrolled synthesis of polyketide libraries.

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