Výsledky vyhledávání - "Eugene V. Genovesi"

Respiratory syncytial virus fusion inhibitors. Part 4: Optimization for oral bioavailability

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 17:895-901

A series of benzimidazole-based inhibitors of respiratory syncytial virus (RSV) fusion were optimized for antiviral potency, membrane permeability and metabolic stability in human liver microsomes. 1-Cyclopropyl-1,3-dihydro-3-[[1-(4-hydroxybutyl)-1H-

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::54f0b15de4e6b963a15896b9c356593f
https://doi.org/10.1016/j.bmcl.2006.11.063

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Respiratory syncytial virus fusion inhibitors. Part 3: Water-soluble benzimidazol-2-one derivatives with antiviral activity in vivo

Autor: Eugene V. Genovesi, Yi Zhang, Ashok K. Trehan, Philip R. Wyde, Ivette Medina, Nicholas A. Meanwell, Kathleen F. Kadow, Xiangdong Alan Wang, Rita L. Civiello, Christopher Cianci, Zhiwei Yin, H. Belgin Gulgeze, Keith D. Combrink, Bradley C. Pearce, Junius Clarke, Lucinda Lamb, Kuo-Long Yu, Mark Krystal

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 16:1115-1122

The introduction of acidic and basic functionality into the side chains of respiratory syncytial virus (RSV) fusion inhibitors was examined in an effort to identify compounds suitable for evaluation in vivo in the cotton rat model of RSV infection fo

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d1e43e7214e5a9a067bd12b1792d30b1
https://doi.org/10.1016/j.bmcl.2005.11.109

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Oral Efficacy of a Respiratory Syncytial Virus Inhibitor in Rodent Models of Infection

Autor: Christopher Cianci, Ny Sin, Junius M. Clark, Lisa Zadjura, Richard J. Colonno, Zhufang Li, Keith D. Combrink, Lucinda Lamb, Ivette Medina, Celia D’Arienzo, Hyekyung Yang, Nicholas A. Meanwell, Kuo-Long Yu, Mark Krystal, Zheng Yang, Eugene V. Genovesi

Publikováno v: Antimicrobial Agents and Chemotherapy. 48:2448-2454

BMS-433771 is a potent inhibitor of respiratory syncytial virus (RSV) replication in vitro. Mechanism of action studies have demonstrated that BMS-433771 halts virus entry through inhibition of F protein-mediated membrane fusion. BMS-433771 also exhi

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5ac8d8e7eb21e74b3bb28819f9ea4659
https://doi.org/10.1128/aac.48.7.2448-2454.2004

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Orally Active Fusion Inhibitor of Respiratory Syncytial Virus

Publikováno v: Antimicrobial Agents and Chemotherapy. 48:413-422

BMS-433771 was found to be a potent inhibitor of respiratory syncytial virus (RSV) replication in vitro. It exhibited excellent potency against multiple laboratory and clinical isolates of both group A and B viruses, with an average 50% effective con

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::cd9c6ed51104037a4bdae59d46b9f982
https://doi.org/10.1128/aac.48.2.413-422.2004

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Antiviral efficacy of lobucavir (BMS-180194), a cyclobutyl-guanosine nucleoside analogue, in the woodchuck (Marmota monax) model of chronic hepatitis B virus (HBV) infection

Autor: Eugene V. Genovesi, S. Innaimo, Lucinda Lamb, D. Taylor, Ivette Medina, Richard J. Colonno, M. Seifer, Junius M. Clark

Publikováno v: Antiviral Research. 48:197-203

Lobucavir (BMS-180194), a cyclobutyl-guanosine nucleoside analogue, effectively reduced WHV-viremia in chronically infected carrier woodchucks (Marmota monax) by daily per os treatment. WHV-viremia in the animals was measured by the serum content of

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::272d72d898103a0f51c9df7a3fa9cf34
https://doi.org/10.1016/s0166-3542(00)00128-5

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Efficacy of the Carbocyclic 2′-Deoxyguanosine Nucleoside BMS-200475 in the Woodchuck Model of Hepatitis B Virus Infection

Autor: Ivette Medina, Junius M. Clark, D. Taylor, S. Innaimo, David N. Standring, Richard J. Colonno, M. Seifer, Lucinda Lamb, Eugene V. Genovesi

Publikováno v: Antimicrobial Agents and Chemotherapy. 42:3209-3217

Human hepatitis B virus (HBV), the prototype member of a small family of hepadnaviruses, is an enveloped DNA virus with a partially double-stranded 3.2-kb circular genome. HBV infection is widespread and is a major cause of human liver disease (4). W

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::999e532f984d5705f5f12213f1cb75c3
https://doi.org/10.1128/aac.42.12.3209

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Respiratory syncytial virus fusion inhibitors. Part 6: an examination of the effect of structural variation of the benzimidazol-2-one heterocycle moiety

Publikováno v: Bioorganicmedicinal chemistry letters. 17(17)

The effect of structural variation of the benzimidazol-2-one ring of RSV fusion inhibitors related to BMS-433771 (1) was examined in conjunction with side chain modifications and the introduction of an aminomethyl substituent at the 5-position of the

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2d06163d4bd52be523754844a67da7d0
https://pubmed.ncbi.nlm.nih.gov/17616396

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Long-term entecavir treatment results in sustained antiviral efficacy and prolonged life span in the woodchuck model of chronic hepatitis infection

Autor: Junius M. Clark, Lawrence Corey, Meei-Li Huang, Richard J. Colonno, Burt Rose, Steven Locarnini, Bud C. Tennant, Lucinda Lamb, Ivette Medina, Margaret Littlejohn, Eugene V. Genovesi, Stephen K. Durham

Publikováno v: The Journal of infectious diseases. 184(10)

Entecavir (ETV) is a guanosine nucleoside analogue with potent antiviral efficacy in woodchucks chronically infected with woodchuck hepatitis virus. To explore the consequences of prolonged virus suppression, woodchucks received ETV orally for 8 week

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::079f9d68766ea641b93d1bb26fe88518
https://pubmed.ncbi.nlm.nih.gov/11679911

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