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Your search keyword '"Mike Westby"' showing total 4 results
Start Over Author "Mike Westby" Journal journal of medicinal chemistry
4 results on '"Mike Westby"'

1. An Imidazopiperidine Series of CCR5 Antagonists for the Treatment of HIV: The Discovery of N-{(1S)-1-(3-Fluorophenyl)-3-[(3-endo)-3-(5-isobutyryl-2-methyl-4,5,6,7-tetrahydro-1H-imidazo[4,5-c]pyridin-1-yl)-8-azabicyclo[3.2.1]oct-8-yl]propyl}acetamide (PF-232798)

Author

Manos Perros, David C. Pryde, Rob Webster, Francesca Perruccio, Michelle Y. Platts, Rhys M. Jones, Deborah Rodrigues, David V. Batchelor, David Ellis, Donald Stuart Middleton, David R. Fenwick, Patrick Dorr, Stupple Paul Anthony, Mike Westby, Anthony Wood, Helen J. Mason, Nicholas Smith, Martin Corless, Sebastien Galan, and Peter T. Stephenson

Subjects
biology, Chemistry, Stereochemistry, Chemokine receptor CCR5, hERG, Antagonist, Stereoisomerism, CCR5 receptor antagonist, Pharmacology, chemistry.chemical_compound, Drug Discovery, biology.protein, Molecular Medicine, Structure–activity relationship, Acetamide, Maraviroc
Abstract

Preventing entry of HIV into human host cells has emerged as an attractive approach to controlling viral replication. Maraviroc 1 is an approved antagonist of the human CCR5 receptor which prevents the entry of HIV. Herein, we report the design and discovery of a series of imidazopiperidine CCR5 antagonists which retain the attractive antiviral profile and window over hERG activity of maraviroc 1, combined with improved absorption profiles in rat and dog. Furthermore, this series of compounds has been shown to retain activity against a laboratory generated maraviroc-resistant HIV-1 strain, which indicates an alternative resistance profile to that of maraviroc 1. Compound 41f (PF-232798) was selected as a clinical candidate from the imidazopiperidine series and is currently in phase II clinical trials.

Published
2010
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2. An imidazopiperidine series of CCR5 antagonists for the treatment of HIV: the discovery of N-{(1S)-1-(3-fluorophenyl)-3-[(3-endo)-3-(5-isobutyryl-2-methyl-4,5,6,7-tetrahydro-1H-imidazo[4,5-c]pyridin-1-yl)-8-azabicyclo[3.2.1]oct-8-yl]propyl}acetamide (PF-232798)

Author

Paul A, Stupple, David V, Batchelor, Martin, Corless, Patrick K, Dorr, David, Ellis, David R, Fenwick, Sébastien R G, Galan, Rhys M, Jones, Helen J, Mason, Donald S, Middleton, Manos, Perros, Francesca, Perruccio, Michelle Y, Platts, David C, Pryde, Deborah, Rodrigues, Nicholas N, Smith, Peter T, Stephenson, Robert, Webster, Mike, Westby, and Anthony, Wood

Subjects
Models, Molecular, ERG1 Potassium Channel, Anti-HIV Agents, Imidazoles, Stereoisomerism, Triazoles, Ether-A-Go-Go Potassium Channels, Cell Line, Rats, Maraviroc, Structure-Activity Relationship, Dogs, Cyclohexanes, Cricetinae, CCR5 Receptor Antagonists, Drug Resistance, Viral, HIV-1, Leukocytes, Mononuclear, Animals, Humans, Azabicyclo Compounds, Protein Binding, Tropanes
Abstract

Preventing entry of HIV into human host cells has emerged as an attractive approach to controlling viral replication. Maraviroc 1 is an approved antagonist of the human CCR5 receptor which prevents the entry of HIV. Herein, we report the design and discovery of a series of imidazopiperidine CCR5 antagonists which retain the attractive antiviral profile and window over hERG activity of maraviroc 1, combined with improved absorption profiles in rat and dog. Furthermore, this series of compounds has been shown to retain activity against a laboratory generated maraviroc-resistant HIV-1 strain, which indicates an alternative resistance profile to that of maraviroc 1. Compound 41f (PF-232798) was selected as a clinical candidate from the imidazopiperidine series and is currently in phase II clinical trials.

Published
2010

3. An Imidazopiperidine Series of CCR5 Antagonists for the Treatment of HIV: The Discovery of N-{(1S)-1-(3-Fluorophenyl)-3-[(3-endo)-3-(5-isobutyryl-2-methyl-4,5,6,7-tetrahydro-1H-imidazo[4,5-c]pyridin-1-yl)-8-azabicyclo[3.2.1]oct-8-yl]propyl}acetamide...

Author

Paul A. Stupple, David V. Batchelor, Martin Corless, Patrick K. Dorr, David Ellis, David R. Fenwick, Sébastien R. G. Galan, Rhys M. Jones, Helen J. Mason, Donald S. Middleton, Manos Perros, Francesca Perruccio, Michelle Y. Platts, David C. Pryde, Deborah Rodrigues, Nicholas N. Smith, Peter T. Stephenson, Robert Webster, Mike Westby, and Anthony Wood

Published
2011
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