Search Results - "Donghi, Monica"
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Discovery of Raltegravir, a Potent, Selective Orally Bioavailable HIV-Integrase Inhibitor for the Treatment of HIV-AIDS Infection
Published in Journal of medicinal chemistry (25-09-2008)“…Human immunodeficiency virus type-1 (HIV-1) integrase is one of the three virally encoded enzymes required for replication and therefore a rational target for…”
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2
A Combinatorial Approach to Polyketide-Type Libraries by Iterative Asymmetric Aldol Reactions Performed on Solid Support
Published in Angewandte Chemie International Edition (15-09-2000)“…Solid‐phase synthesis of polyketide‐type sequences, such as 1, can be achieved efficiently by iterative, boron‐mediated, aldol reactions of chiral ketones 2…”
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3
Synthesis of a hexahydropyrimido[1,2- a]azepine-2-carboxamide derivative useful as an HIV integrase inhibitor
Published in Tetrahedron letters (19-11-2007)“…The hexahydropyrimido[1,2- a]azepine-2-carboxamide derivative 1 could be obtained by three synthetic strategies, which allowed access to multigram amounts of…”
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4
3-Hydroxy-4-oxo-4H-pyrido[1,2-a]pyrimidine-2-carboxylates-A new class of HIV-1 integrase inhibitors
Published in Bioorganic & medicinal chemistry letters (01-04-2009)Get full text
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Taxol Semisynthesis: A Highly Enantio- and Diastereoselective Synthesis of the Side Chain and a New Method for Ester Formation at C-13 Using Thioesters
Published in Journal of organic chemistry (11-07-1997)“…A very simple, new, and straightforward approach to the Paclitaxel (Taxol) and Docetaxel (Taxotere) side chains has been developed using the imine addition…”
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6
3-Hydroxy-4-oxo-4H-pyrido[1,2-a]pyrimidine-2-carboxylates--a new class of HIV-1 integrase inhibitors
Published in Bioorganic & medicinal chemistry letters (01-04-2009)“…A new class of inhibitors of HIV-1 integrase has been optimized to provide selective and highly efficient strand transfer inhibition…”
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7
Phosphoramidate Prodrugs of 2′-C-Methylcytidine for Therapy of Hepatitis C Virus Infection
Published in Journal of medicinal chemistry (10-09-2009)“…The application of a phosphoramidate prodrug approach to 2′-C-methylcytidine (NM107), the first nucleoside inhibitor of the hepatitis C virus (HCV) NS5B…”
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8
3-Hydroxy-4-oxo-4 H-pyrido[1,2- a]pyrimidine-2-carboxylates—A new class of HIV-1 integrase inhibitors
Published in Bioorganic & medicinal chemistry letters (2009)“…The synthesis and SAR of a new class of HIV-1 integrase inhibitors is reported. A new class of inhibitors of HIV-1 integrase has been optimized to provide…”
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9
Allosteric inhibitors of hepatitis C virus NS5B polymerase thumb domain site II: Structure-based design and synthesis of new templates
Published in Bioorganic & medicinal chemistry (15-04-2010)“…Chronic hepatitis C virus (HCV) infections are a significant medical problem worldwide. The NS5B Polymerase of HCV plays a central role in virus replication…”
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10
Design and Synthesis of Bicyclic Pyrimidinones as Potent and Orally Bioavailable HIV-1 Integrase Inhibitors
Published in Journal of medicinal chemistry (28-02-2008)“…HIV integrase is one of the three enzymes encoded by HIV genome and is essential for viral replication, but integrase inhibitors as marketed drugs have just…”
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11
Synthesis and evaluation of novel phosphoramidate prodrugs of 2′-methyl cytidine as inhibitors of hepatitis c virus NS5B polymerase
Published in Bioorganic & medicinal chemistry letters (01-03-2009)“…The synthesis and SAR of phosphoramidate prodrugs of 2′-methyl cytidine as inhibitors of HCV NS5B polymerase is reported. A variety of new prodrugs of…”
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12
3-Hydroxy-4-oxo-4H-pyrido[1,2-a]pyrimidine-2-carboxylates—fast access to a heterocyclic scaffold for HIV-1 integrase inhibitors
Published in Tetrahedron letters (10-11-2008)“…An efficient and reliable synthesis of the heterocyclic scaffold methyl- 3-hydroxy-4-oxo-4H-pyrido[1,2-a]pyrimidine-2-carboxylate is described. The scope of…”
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13
Inhibitors of the Hepatitis C Virus NS3 Protease with Basic Amine Functionality at the P3-Amino Acid N-Terminus: Discovery and Optimization of a New Series of P2−P4 Macrocycles
Published in Journal of medicinal chemistry (13-08-2009)“…In a follow-up to our recent disclosure of P2−P4 macrocyclic inhibitors of the hepatitis C virus (HCV) NS3 protease (e.g., 1, Chart 1), we report a new but…”
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14
3-Hydroxy-4-oxo-4 H-pyrido[1,2- a]pyrimidine-2-carboxylates—fast access to a heterocyclic scaffold for HIV-1 integrase inhibitors
Published in Tetrahedron letters (2008)“…An efficient and reliable synthesis of the heterocyclic scaffold methyl-3-hydroxy-4-oxo-4 H-pyrido[1,2- a]pyrimidine-2-carboxylate is described. The scope of…”
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15
Structure-based design of amidinophenylurea-derivatives for factor VIIa inhibition
Published in Bioorganic & medicinal chemistry letters (16-07-2004)“…The amidinophenylurea scaffold was earlier shown to provide an excellent template for the synthesis of novel and potent inhibitors of the blood coagulation…”
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16
Stereocontrolled synthesis of polyketide libraries: Boron-mediated aldol reactions with aldehydes on solid support
Published in Tetrahedron (03-12-1998)“…Two complementary classes of chiral boron enolates for adaptation to aldol additions to resin-bound aldehydes were studied: ( i) the thioester-derived enolate…”
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17
A Combinatorial Approach to Polyketide-Type Libraries by Iterative Asymmetric Aldol Reactions Performed on Solid Support
Published in Angewandte Chemie (15-09-2000)“…Die Festphasensynthese von Polyketidsequenzen vom Typ 1 gelang durch iterative, Bor‐vermittelte Aldolreaktionen des chiralen Ketons 2 mit dem auf einem…”
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