18 results on '"Ozkan Sari"'
Search Results
2. Erratum for Amblard et al., 'Novel Hepatitis B Virus Capsid Assembly Modulator Induces Potent Antiviral Responses In Vitro and in Humanized Mice'
- Author
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Zhe Chen, Maud Boussand, Virgile Rat, Leda Bassit, Olivia Ollinger Russell, Ozkan Sari, Sijia Tao, Hugues de Rocquigny, Sebastien Boucle, Helene Strick-Marchand, Kiran Verma, Franck Amblard, James P. Di Santo, Oriane Fiquet, Tugba Ozturk, Bryan Cox, and Raymond F. Schinazi
- Subjects
Pharmacology ,Hepatitis B virus ,Infectious Diseases ,Capsid ,Chemistry ,medicine ,Pharmacology (medical) ,medicine.disease_cause ,Virology ,In vitro - Published
- 2020
3. Novel Hepatitis B Virus Capsid Assembly Modulator Induces Potent Antiviral Responses In Vitro and in Humanized Mice
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Maud Boussand, Leda Bassit, Oriane Fiquet, Franck Amblard, Virgile Rat, Sijia Tao, Sebastien Boucle, Zhe Chen, Hugues de Rocquigny, Olivia Ollinger Russell, Bryan Cox, Ozkan Sari, Kiran Verma, Helene Strick-Marchand, Raymond F. Schinazi, Tugba Ozturk, James P. Di Santo, Strick-Marchand, Helene, Pathogen COinfection:HIV, Tuberculosis, Malaria and Hepatitis C virus - PATHCO - - EC:FP7:HEALTH2012-11-01 - 2017-10-31 - 305578 - VALID, Emory University School of Medicine, Emory University [Atlanta, GA], Morphogénèse et antigénicité du VIH et du virus des Hépatites (MAVIVH - U1259 Inserm - CHRU Tours ), Centre Hospitalier Régional Universitaire de Tours (CHRU Tours)-Université de Tours (UT)-Institut National de la Santé et de la Recherche Médicale (INSERM), Immunité Innée - Innate Immunity, Institut Pasteur [Paris] (IP)-Institut National de la Santé et de la Recherche Médicale (INSERM), This work was supported in part by NIH Grant 1-R01-AI-132833(RFS), and 5P30-AI-50409 (CFAR)(RFS), by Agence Nationale de Recherches sur le Sida et les Hépatites Virales (ANRS) Grants #2016-16180 and #2016-16365, European Commission Seventh Framework Programme PATHCo(HEALTH-F3-2012-305578), Institut Pasteur, and Institut national de la santé et de la recherche médicale (HSM), by ANRS and Institut national de la santé et de la recherche médicale (INSERM) (HDR)., European Project: 305578,EC:FP7:HEALTH,FP7-HEALTH-2012-INNOVATION-1,PATHCO(2012), Université de Tours-Institut National de la Santé et de la Recherche Médicale (INSERM)-Centre Hospitalier Régional Universitaire de Tours (CHRU TOURS), Institut Pasteur [Paris]-Institut National de la Santé et de la Recherche Médicale (INSERM), and Institut National de la Santé et de la Recherche Médicale (INSERM)-Institut Pasteur [Paris]
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viruses ,[CHIM.THER]Chemical Sciences/Medicinal Chemistry ,medicine.disease_cause ,Mice ,0302 clinical medicine ,Interferon ,capsid ,Pharmacology (medical) ,[SDV.MP.VIR] Life Sciences [q-bio]/Microbiology and Parasitology/Virology ,0303 health sciences ,Mice, Inbred BALB C ,Entecavir ,cccDNA ,Hepatitis B ,antiviral ,3. Good health ,Infectious Diseases ,HBeAg ,[SDV.MP.VIR]Life Sciences [q-bio]/Microbiology and Parasitology/Virology ,Microsomes, Liver ,030211 gastroenterology & hepatology ,DNA, Circular ,Erratum ,Viral load ,medicine.drug ,Guanine ,[CHIM.THER] Chemical Sciences/Medicinal Chemistry ,Biology ,Antiviral Agents ,Hepatitis B Antigens ,03 medical and health sciences ,Dogs ,medicine ,Animals ,Humans ,Hepatitis B Vaccines ,Nucleocapsid ,030304 developmental biology ,Pharmacology ,Hepatitis B virus ,Hepatitis B Surface Antigens ,Nucleoside analogue ,Virus Assembly ,Virology ,digestive system diseases ,Rats ,Humanized mouse ,Hepatocytes ,hepatitis B virus - Abstract
International audience; Hepatitis B virus (HBV) affects an estimated 250 million chronic carriers worldwide. Though several vaccines exist, they are ineffective for those already infected. HBV persists due to the formation of covalently closed circular DNA (cccDNA)-the viral minichromosome-in the nucleus of hepatocytes. Current nucleoside analogs and interferon therapies rarely clear cccDNA, requiring lifelong treatment. Our group identified GLP-26, a novel glyoxamide derivative that alters HBV nucleocapsid assembly and prevents viral DNA replication. GLP-26 exhibited single-digit nanomolar anti-HBV activity, inhibition of HBV e antigen (HBeAg) secretion, and reduced cccDNA amplification, in addition to showing a promising preclinical profile. Strikingly, long term combination treatment with entecavir in a humanized mouse model induced a decrease in viral loads and viral antigens that was sustained for up to 12 weeks after treatment cessation.
- Published
- 2020
4. Discovery of a Series of 2'-α-Fluoro,2'-β-bromo-ribonucleosides and Their Phosphoramidate Prodrugs as Potent Pan-Genotypic Inhibitors of Hepatitis C Virus
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Tamara R. McBrayer, Biing Y. Lin, Kiran Verma, Ozkan Sari, Olivia Ollinger Russell, Judy Pattassery, Yong Jiang, Maria Luz G. Pascual, Steven J. Coats, Seema Mengshetti, Leda Bassit, Jong Hyun Cho, Reuben Ovadia, Sijia Tao, Sam Lee, Mahesh Kasthuri, Robert A. Domaoal, Tony Whitaker, Coralie De Schutter, Raymond F. Schinazi, Longhu Zhou, Lothar Uher, Hongwang Zhang, Maryam Ehteshami, and Franck Amblard
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Male ,Hepatitis C virus ,Deoxyribonucleosides ,Hepacivirus ,Viral Nonstructural Proteins ,medicine.disease_cause ,01 natural sciences ,Antiviral Agents ,Article ,03 medical and health sciences ,Dogs ,Pharmacokinetics ,Cell Line, Tumor ,Drug Discovery ,medicine ,Animals ,Humans ,Prodrugs ,Enzyme Inhibitors ,Polymerase ,030304 developmental biology ,0303 health sciences ,biology ,Chemistry ,Drug discovery ,Phosphoramidate ,Prodrug ,0104 chemical sciences ,010404 medicinal & biomolecular chemistry ,Biochemistry ,Microsome ,biology.protein ,Microsomes, Liver ,Molecular Medicine ,Deoxyuracil Nucleotides ,Nucleoside - Abstract
Hepatitis C virus (HCV) nucleoside inhibitors display pan-genotypic activity, a high barrier to the selection of resistant virus, and are some of the most potent direct-acting agents with durable sustained virologic response in humans. Herein, we report, the discovery of β-d-2'-Br,2'-F-uridine phosphoramidate diastereomers 27 and 28, as nontoxic pan-genotypic anti-HCV agents. Extensive profiling of these two phosphorous diastereomers was performed to select one for in-depth preclinical profiling. The 5'-triphosphate formed from these phosphoramidates selectively inhibited HCV NS5B polymerase with no inhibition of human polymerases and cellular mitochondrial RNA polymerase up to 100 μM. Both are nontoxic by a variety of measures and display good stability in human blood and favorable metabolism in human intestinal microsomes and liver microsomes. Ultimately, a preliminary oral pharmacokinetics study in male beagles showed that 28 is superior to 27 and is an attractive candidate for further studies to establish its potential value as a new clinical anti-HCV agent.
- Published
- 2019
5. Discovery and structure activity relationship of glyoxamide derivatives as anti-hepatitis B virus agents
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Franck Amblard, Bryan Cox, Tugba Ozturk, Sebastien Boucle, Raymond F. Schinazi, Olivia Ollinger-Russell, Zhe Chen, Kiran Verma, Ozkan Sari, and Leda Bassit
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Hepatitis B virus ,Clinical Biochemistry ,Pharmaceutical Science ,Microbial Sensitivity Tests ,medicine.disease_cause ,Antiviral Agents ,Biochemistry ,Article ,Structure-Activity Relationship ,Drug Discovery ,medicine ,Structure–activity relationship ,Secretion ,Molecular Biology ,Dose-Response Relationship, Drug ,Molecular Structure ,Chemistry ,Organic Chemistry ,cccDNA ,Virology ,Sulfonylurea Compounds ,Capsid ,HBeAg ,Humanized mouse ,Molecular Medicine ,Viral load - Abstract
Chronic hepatitis B viral infection is a significant health problem world-wide, and currently available antiviral agents suppress HBV infections, but rarely cure this disease. It is presumed that antiviral agents that target the viral nuclear reservoir of transcriptionally active cccDNA may eliminate HBV infection. Through a series of chemical optimization, we identified a new series of glyoxamide derivatives affecting HBV nucleocapsid formation and cccDNA maintenance at low nanomolar levels. Among all the compounds synthesized, GLP-26 displays a major effect on HBV DNA, HBeAg secretion and cccDNA amplification. In addition, GLP-26 shows a promising pre-clinical profile and long-term effect on viral loads in a humanized mouse model.
- Published
- 2021
6. Sonication-Assisted Synthesis of(E)-2-Methyl-but-2-enyl Nucleoside Phosphonate Prodrugs
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Andrzej J. Bojarski, Vincent Roy, Robert Snoeck, Raymond F. Schinazi, Maxime Bessières, Dawid Warszycki, Graciela Andrei, Ozkan Sari, Steven P. Nolan, and Luigi A. Agrofoglio
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Olefin fiber ,010405 organic chemistry ,Stereochemistry ,RNA ,General Chemistry ,Prodrug ,010402 general chemistry ,Metathesis ,Pivaloyloxymethyl ,01 natural sciences ,Phosphonate ,0104 chemical sciences ,chemistry.chemical_compound ,chemistry ,Nucleoside ,DNA - Abstract
Several hitherto unknown acyclic 2-methyl-but-2-enyl nucleoside phosphonate analogs (ANPs) and their bis-(pivaloyloxymethyl) prodrug forms were prepared by a challenging ultrasonic-assisted olefin cross metathesis and further modifications under microwaves, giving rise to a small library of title compounds. These ANPs were evaluated against a wide spectrum of DNA/RNA viruses. Among them, the most active compound exhibited a micromolar anti-HIV-1 activity with an EC50 of 1.1 µM and an EC90 of 4.2 µM.
- Published
- 2016
7. Synthesis of (2S)-2-Chloro-2-fluororibolactone via Stereoselective Electrophilic Fluorination
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Franck Amblard, Raymond F. Schinazi, Coralie De Schutter, Steven J. Coats, and Ozkan Sari
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Molecular Structure ,010405 organic chemistry ,Chemistry ,Organic Chemistry ,Electrophilic fluorination ,Stereoisomerism ,Fluorine ,010402 general chemistry ,01 natural sciences ,Article ,0104 chemical sciences ,Lactones ,Yield (chemistry) ,Organic chemistry ,Stereoselectivity - Abstract
A novel and efficient route for the preparation of (2S)-2-chloro-2-fluorolactone 29 is described. This approach takes advantage of a highly efficient diastereoselective electrophilic fluorination reaction (94% yield; >50:1 dr)
- Published
- 2017
8. Synthesis of sulfamoylbenzamide derivatives as HBV capsid assembly effector
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Franck Amblard, Olivia Ollinger Russell, Leda Bassit, Bryan Cox, Ozkan Sari, Tugba Ozturk, Sebastien Boucle, and Raymond F. Schinazi
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0301 basic medicine ,Models, Molecular ,HBV RNA encapsidation signal epsilon ,Hepatitis B virus ,030106 microbiology ,Cell ,Microbial Sensitivity Tests ,Antiviral Agents ,Article ,03 medical and health sciences ,Structure-Activity Relationship ,Capsid ,Drug Discovery ,Chlorocebus aethiops ,medicine ,Animals ,Humans ,Secretion ,Binding site ,Vero Cells ,Cells, Cultured ,Cell Proliferation ,Pharmacology ,Dose-Response Relationship, Drug ,Molecular Structure ,Chemistry ,Effector ,Virus Assembly ,Organic Chemistry ,virus diseases ,General Medicine ,cccDNA ,Molecular biology ,digestive system diseases ,030104 developmental biology ,medicine.anatomical_structure ,HBeAg ,Benzamides - Abstract
The synthesis of novel series of sulfamoylbenzamides as HBV capsid assembly effector is reported. The structure was divided into five parts which were independently modified as part of our lead optimization. All synthesized compounds were evaluated for their anti-HBV activity and toxicity in human hepatocytes, lymphocytes and other cells. Additionally, we assessed their effect on HBV cccDNA formation in an HBeAg reporter cell-based assay. Among the 27 compounds reported, several analogs exhibited submicromolar activities and significant reduction of HBeAg secretion. Selected compounds were studied under negative-stain electron microscopy for their ability to disrupt the HBV capsid formation. Structures were modeled into a binding site recently identified in the HBV capsid protein for similar molecules to rationalize the structure-activity relationships for this family of compounds.
- Published
- 2017
9. Synthesis and antiviral evaluation of 2′,2′,3′,3′-tetrafluoro nucleoside analogs
- Author
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Tamara R. McBrayer, Bryan Cox, A. Louise McCormick, Steven J. Coats, Christina Gavegnano, Ozkan Sari, Franck Amblard, Leda Bassit, and Raymond F. Schinazi
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Nucleoside analogue ,010405 organic chemistry ,Chemistry ,Stereochemistry ,Organic Chemistry ,RNA ,virus diseases ,Phosphoramidate ,Prodrug ,010402 general chemistry ,01 natural sciences ,Biochemistry ,Article ,0104 chemical sciences ,Nucleobase ,chemistry.chemical_compound ,Drug Discovery ,Ribose ,medicine ,Moiety ,DNA ,medicine.drug - Abstract
Herein, we report the synthesis of novel 2',2',3',3'-tetrafluorinated nucleoside analogs along with their phosphoramidate prodrugs. A tetrafluoro ribose moiety was coupled with different Boc/benzoyl-protected nucleobases under Mitsunobu conditions. After deprotection, tetrafluorinated nucleosides 13b, 14b, 20b-22b were reacted with phenyl-(isopropoxy-L-alaninyl)-phosphorochloridate to afford corresponding monophosphate prodrugs 24b-28b. All synthesized compounds were evaluated against several DNA and RNA viruses including HIV, HBV, HCV, Ebola and Zika viruses.
- Published
- 2017
10. ChemInform Abstract: Sonication-Assisted Synthesis of (E)-2-Methyl-but-2-enyl Nucleoside Phosphonate Prodrugs
- Author
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Maxime Bessières, Graciela Andrei, Dawid Warszycki, Ozkan Sari, Steven P. Nolan, Luigi A. Agrofoglio, Andrzej J. Bojarski, Robert Snoeck, Raymond F. Schinazi, and Vincent Roy
- Subjects
chemistry.chemical_compound ,Olefin fiber ,chemistry ,RNA ,General Medicine ,Prodrug ,Metathesis ,Pivaloyloxymethyl ,Phosphonate ,Nucleoside ,Combinatorial chemistry ,DNA - Abstract
Several hitherto unknown acyclic 2-methyl-but-2-enyl nucleoside phosphonate analogs (ANPs) and their bis-(pivaloyloxymethyl) prodrug forms were prepared by a challenging ultrasonic-assisted olefin cross metathesis and further modifications under microwaves, giving rise to a small library of title compounds. These ANPs were evaluated against a wide spectrum of DNA/RNA viruses. Among them, the most active compound exhibited a micromolar anti-HIV-1 activity with an EC50 of 1.1 µM and an EC90 of 4.2 µM.
- Published
- 2016
11. The Preparation of Trisubstituted Alkenyl Nucleoside Phosphonates under Ultrasound-Assisted Olefin Cross-Metathesis
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Ozkan Sari, Steven P. Nolan, Luigi A. Agrofoglio, Vincent Roy, and Manabu Hamada
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Olefin fiber ,Molecular Structure ,Chemistry ,Organic Chemistry ,Organophosphonates ,Regioselectivity ,Nucleosides ,Stereoisomerism ,Alkenes ,Ultrasound assisted ,Metathesis ,Biochemistry ,Combinatorial chemistry ,Catalysis ,Physical and Theoretical Chemistry ,Nucleoside - Abstract
Intermolecular ultrasound-assisted olefin cross-metathesis is reported. This approach allows an easy access to challenging trisubstituted alkenyl nucleoside phosphonates. Regioselective chemoenzymatic deacetylation and Mitsunobu coupling are also described.
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- 2013
12. Modifications of Nucleosides, Nucleotides, and Nucleic Acids using Huisgen's [3+2] Azide-Alkyne Cycloaddition: Opening Pandora's Box
- Author
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Sebastien Boucle, Franck Amblard, Ahmed Khalil, Raymond F. Schinazi, and Ozkan Sari
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chemistry.chemical_classification ,chemistry.chemical_compound ,Bioconjugation ,Chemistry ,Stereochemistry ,Oligonucleotide ,Nucleic acid ,Alkyne ,Nucleotide ,Azide ,Nucleoside ,Cycloaddition - Published
- 2016
13. Synthesis and antiviral evaluation of C5-substituted-(1,3-diyne)-2′-deoxyuridines
- Author
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Luigi A. Agrofoglio, Graciela Andrei, Robert Snoeck, Ozkan Sari, Jan Balzarini, and Vincent Roy
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Sindbis virus ,viruses ,Viral transformation ,Chemistry Techniques, Synthetic ,Virus Replication ,medicine.disease_cause ,Antiviral Agents ,Virus ,Cell Line ,HeLa ,Inhibitory Concentration 50 ,chemistry.chemical_compound ,Drug Discovery ,medicine ,Humans ,Pharmacology ,biology ,Chemistry ,Organic Chemistry ,General Medicine ,biology.organism_classification ,Deoxyuridine ,Virology ,Herpes simplex virus ,Viral replication ,Viruses ,Vero cell - Abstract
Starting from acetylated 5-ethynyl-2'-deoxyuridine (3), 14 hitherto unknown C5-substituted-(1,3-diyne)-2'-deoxyuridines (with cyclopropyl, hydroxymethyl, methylcyclopentane, p-(substituted)phenyl and disubstituted-phenyl substituents) have been synthesized via a nickel-copper catalyzed C-H activation between two terminal alkynes, in yields ranging from 19% to 67%. Their antiviral activities were measured against a large number of DNA and RNA viruses including herpes simplex virus type 1 and type 2, varicella-zoster virus, human cytomegalovirus and vaccinia virus. The 5-[4-(4-trifluoromethoxyphenyl)buta-1,3-diynyl]-2'-deoxyuridine (26) is the most potent inhibitor of this series against VZV with an EC(50) of ~1 μM and a CC(50) of 55 μM. Their cytostatic activities were determined against murine leukemia cells, human T-lymphocyte cells and cervix carcinoma cells. Compounds were also evaluated on a wide panel of RNA viruses, including influenza virus A (H1N1 and H3N2) and B in MDCK cell cultures, parainfluenza-3 virus, reovirus-1, Sindbis virus and Punta Toro virus in Vero cell cultures and vesicular stomatitis, coxsackie B4 and respiratory syncytial virus in HeLa cell cultures and against human immunodeficiency virus type 1 and 2 in CEM cell cultures, with no specific antiviral effect. This class of compounds could be of further interest for lead optimization as anti-infectious (i.e. herpetic) agents.
- Published
- 2012
14. Synthesis of dihydropyrimidine α,γ-diketobutanoic acid derivatives targeting HIV integrase
- Author
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Ozkan Sari, Stéphane Bourg, Pascal Bonnet, Christophe Marchand, Mathieu Métifiot, Vincent Roy, Raymond F. Schinazi, Yves Pommier, Luigi A. Agrofoglio, Emory University School of Medicine, Emory University [Atlanta, GA], Centre de Recherches sur les Fonctionnements et Dysfonctionnements Psychologiques (CRFDP), Université de Rouen Normandie (UNIROUEN), Normandie Université (NU)-Normandie Université (NU)-Institut de Recherche Interdisciplinaire Homme et Société (IRIHS), Normandie Université (NU)-Normandie Université (NU)-Université de Rouen Normandie (UNIROUEN), Normandie Université (NU), Laboratory of Molecular Pharmacology, National Institutes of Health [Bethesda] (NIH)-National Cancer Institute [Bethesda] (NCI-NIH), National Institutes of Health [Bethesda] (NIH), Laboratoire de génie électrique de Paris (LGEP), Université Paris-Sud - Paris 11 (UP11)-Université Pierre et Marie Curie - Paris 6 (UPMC)-Ecole Supérieure d'Electricité - SUPELEC (FRANCE)-Centre National de la Recherche Scientifique (CNRS), Institut de Chimie Organique et Analytique (ICOA), Commissariat à l'énergie atomique et aux énergies alternatives (CEA)-Université d'Orléans (UO)-Institut National de la Santé et de la Recherche Médicale (INSERM)-Institut de Chimie du CNRS (INC)-Centre National de la Recherche Scientifique (CNRS), Global Virus Network, University of South Florida [Tampa] (USF), Institut de Recherche Interdisciplinaire Homme et Société (IRIHS), and Université d'Orléans (UO)-Centre National de la Recherche Scientifique (CNRS)-Commissariat à l'énergie atomique et aux énergies alternatives (CEA)-Institut de Chimie du CNRS (INC)-Institut National de la Santé et de la Recherche Médicale (INSERM)
- Subjects
Models, Molecular ,Stereochemistry ,Anti-HIV Agents ,Cell Survival ,HIV Integrase ,[CHIM.THER]Chemical Sciences/Medicinal Chemistry ,Article ,chemistry.chemical_compound ,Structure-Activity Relationship ,Cell Line, Tumor ,Drug Discovery ,Chlorocebus aethiops ,Structure–activity relationship ,Moiety ,Animals ,Humans ,Chelation ,HIV Integrase Inhibitors ,Cytotoxicity ,Vero Cells ,ComputingMilieux_MISCELLANEOUS ,Cell Proliferation ,Pharmacology ,biology ,Dose-Response Relationship, Drug ,Molecular Structure ,Aryl ,Organic Chemistry ,Active site ,General Medicine ,Prodrug ,3. Good health ,Integrase ,Pyrimidines ,chemistry ,biology.protein ,HIV-1 ,Butyric Acid - Abstract
The synthesis and antiviral evaluation of a series of dihydropyrimidinone and thiopyrimidine derivatives bearing aryl α,γ-diketobutanoic acid moiety are described using the Biginelli multicomponent reaction as key step. The most active among 20 synthesized novel compounds were 4c, 4d and 5b, which possess nanomolar HIV-1 integrase (IN) stand transfer (ST) inhibition activities. In order to understand their mode of interactions within the IN active site, we docked all the compounds into the previously reported X-ray crystal structure of IN. We observed that compounds 4c, 4d and 5b occupied an area close to the two catalytic Mg(2+) ions surrounded by their chelating triad (E221, D128 and D185), DC16, Y212 and the β-diketo acid moiety of 4c, 4d and 5b chelating Mg(2+). As those compounds lack anti-HIV activities in cell, their prodrugs were synthetized. The prodrug 4c' exhibited an anti-HIV activity of 0.19 μM in primary human lymphocytes with some cytotoxicity. All together, these results indicate that the new analogs potentially interact within the catalytic site with highly conserved residues important for IN catalytic activity.
- Published
- 2015
15. Bug Prediction for an ATM Monitoring Software - Use of Logistic Regression Analysis for Bug Prediction
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Oya Kalipsiz and Ozkan Sari
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business.industry ,Computer science ,computer.software_genre ,Software quality ,Software sizing ,parasitic diseases ,Regression testing ,Software construction ,Software quality analyst ,Software verification and validation ,Data mining ,Software reliability testing ,Software regression ,Software engineering ,business ,computer - Abstract
Software testing which is carried out for the elimination of the software defects is one of the significant activities to achieve software quality. However, testing each fragment of the software is impossible and defects still occur even after several detailed test activities. Therefore, there is a need for effective methods to detect bugs in software. It is possible to detect faulty portions of the code earlier by examining the characteristics of the code. Serving this purpose, bug prediction activities help to detect the presence of defects as early as possible in an automated fashion. As a part of the ongoing thesis study, an effective model is aimed to be developed in order to predict software entities having bugs. A public bug database and ATM monitoring software source code are used for the creation of the model and to find the performance of the study.
- Published
- 2015
16. Nucleosides Modified at the Base Moiety
- Author
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Ozkan Sari, Vincent Roy, and Luigi A. Agrofoglio
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Chemistry ,Stereochemistry ,Moiety ,Base (exponentiation) ,Antibacterial activity - Published
- 2013
17. ChemInform Abstract: Synthesis and Antiviral Evaluation of C5-Substituted-(1,3-diyne)-2′-deoxyuridines
- Author
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Graciela Andrei, Luigi A. Agrofoglio, Robert Snoeck, Vincent Roy, Jan Balzarini, and Ozkan Sari
- Subjects
Terminal (electronics) ,Chemistry ,Stereochemistry ,Nucleic acid ,General Medicine - Abstract
Fourteen hitherto unknown title compounds are synthesized using a Ni—Cu cocatalyzed C-H activation of two terminal alkynes as key step.
- Published
- 2012
18. Synthesis and antiviral evaluation of bis(POM) prodrugs of (E)-[4'-phosphono-but-2'-en-1'-yl]purine nucleosides
- Author
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Robert Snoeck, Manabu Hamada, Jan Balzarini, Luigi A. Agrofoglio, Vincent Roy, Ugo Pradere, Aurélien Montagu, Graciela Andrei, and Ozkan Sari
- Subjects
Purine ,Stereochemistry ,viruses ,Organophosphonates ,Viral Plaque Assay ,medicine.disease_cause ,Antiviral Agents ,Nucleobase ,Madin Darby Canine Kidney Cells ,chemistry.chemical_compound ,Dogs ,Chlorocebus aethiops ,Drug Discovery ,medicine ,Animals ,Humans ,RNA Viruses ,Prodrugs ,Vero Cells ,Pharmacology ,Organic Chemistry ,Synthon ,Varicella zoster virus ,DNA Viruses ,virus diseases ,General Medicine ,Purine Nucleosides ,Prodrug ,Phosphonate ,chemistry ,Drug Design ,Mitsunobu reaction ,DNA ,HeLa Cells - Abstract
Seventeen hitherto unknown bis(POM) prodrugs of novel (E)-[4'-phosphono-but-2'-en-1'-yl]purine nucleosides were prepared in a straight approach and at good yields. Those compounds were synthesized by the reaction of purine nucleobases directly with the phosphonate synthon 3 bearing POM biolabile groups under Mitsunobu conditions. All obtained compounds were evaluated for their antiviral activities against a large number of DNA and RNA viruses including herpes simplex viruses 1 and 2, varicella zoster virus, Feline herpes virus, human cytomegalovirus, HIV-1 and HIV-2. Among these molecules, some of them exhibit anti-VZV and anti-HIV activity at submicromolar concentrations. This class of compound will be of further interest for lead optimization as anti-infectious agents.
- Published
- 2012
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