Výsledky vyhledávání - "Keith D. Combrink"

Rifamycin derivatives active against pathogenic rapidly-growing mycobacteria

Autor: Bryant De Jesus, Sebastian Schmidl, Andrea Ramirez Ramos, Petronilo Morin, Stephanie Spring, Florian P. Maurer, Kira Elizondo, Keith D. Combrink

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 29:2112-2115

Infections due to rapidly growing mycobacteria (RGM), and in particular the RGM species Mycobacterium abscessus (Mab), are very difficult to treat and reports on novel therapeutic options are scarce. A hallmark of all pathogenic RGM species is their

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::284da21f64152ac9089bab36be3f4986
https://doi.org/10.1016/j.bmcl.2019.07.001

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Structure-based design and optimization of potent inhibitors of the adenoviral protease

Autor: Samu Melkko, N. Jarousse, David Archer Ellis, Finton Sirockin, A. Bernardi, Aengus Mac Sweeney, Paul Erbel, Paul Ramage, Philipp Grosche, Eva Altmann, Keith D. Combrink, Nicola Hughes

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 25:438-443

Adenoviral infections are associated with a wide range of acute diseases, among which ocular viral conjunctivitis (EKC) and disseminated disease in immunocompromised patients. To date, no approved specific anti-adenoviral drug is available, but there

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0f3777095530490cc9447027eeafc558
https://doi.org/10.1016/j.bmcl.2014.12.057

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Discovery and Structure-Based Optimization of Adenain Inhibitors

Autor: Eva Altmann, A. Bernardi, Paul Erbel, Aengus Mac Sweeney, N. Jarousse, Paul Ramage, Philipp Grosche, Keith D. Combrink, Nicola Hughes, David Archer Ellis, Samu Melkko, Finton Sirockin

Publikováno v: ACS Medicinal Chemistry Letters. 5:937-941

The cysteine protease adenain is the essential protease of adenovirus and, as such, represents a promising target for the treatment of ocular and other adenoviral infections. Through a concise two-pronged hit discovery approach we identified tetrapep

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c8c6b52f270b5d23e3714c30285f506a
https://doi.org/10.1021/ml500224t

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In vivo optimization of 2,3-diaminopyrazine Rho Kinase inhibitors for the treatment of glaucoma

Autor: Abdelmoula Namil, Mark R. Hellberg, Andrew Rusinko, Bryon S. Severns, Jennifer Ward, Colene Drace, Iok-Hou Pang, Shenouda Yacoub, Keith D. Combrink, Curtis R. Kelly, Byron Li, Marsha A. McLaughlin, Raj Patil, N.A. Sharif, Hwang Hsing Chen

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 24:1875-1879

A series of 2,3,6-pyrazine Rho Kinase inhibitors were optimized for in vivo activity for topical ocular dosing. Modifications of the 2-(piperazin-1-yl)pyrazine derivatives produced compounds with improved solubility and physicochemical properties. Mo

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d182bc1267668fdba6283e228caac75f
https://doi.org/10.1016/j.bmcl.2014.03.017

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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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Respiratory syncytial virus inhibitors. Part 2: Benzimidazol-2-one derivatives

Autor: Christopher Cianci, Bradley C. Pearce, Rita L. Civiello, Ashok K. Trehan, Xiangdong Alan Wang, Zhiwei Yin, Keith D. Combrink, Kuo-Long Yu, H. Belgin Gulgeze, Mark Krystal, Nicholas A. Meanwell, Kathleen F. Kadow, Yi Zhang

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 14:1133-1137

Structure-activity relationships for a series of benzimidazol-2-one-based inhibitors of respiratory syncytial virus are described. These studies focused on structural variation of the benzimidazol-2-one substituent, a vector inaccessible in a series

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1cfff2dbeb42fc4e8bdb3945293f2de0
https://doi.org/10.1016/j.bmcl.2003.12.072

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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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