Publication
Title
Selection of a respiratory syncytial virus fusion inhibitor clinical candidate: 2: discovery of a morpholinopropylaminobenzimidazole derivative (TMC353121)
Author
Abstract
A preceding paper (Bonfanti et al. J. Med Chem. 2007, 50, 4572−4584) reported the optimization of the pharmacokinetic profile of substituted benzimidazoles by reducing their tissue retention. However, the modifications that were necessary to achieve this goal also led to a significant drop in anti-RSV activity. This paper describes a molecular modeling study followed by a lead optimization program that led to the recovery of the initial potent antiviral activity and the selection of TMC353121 as a clinical candidate.
Language
English
Source (journal)
Journal of medicinal chemistry. - Washington, D.C., 1963, currens
Publication
Washington, D.C. : 2008
ISSN
0022-2623
Volume/pages
51:4(2008), p. 875-896
ISI
000253353800019
Full text (Publisher's DOI)
UAntwerpen
Faculty/Department
Research group
Publication type
Subject
Affiliation
Publications with a UAntwerp address
External links
Web of Science
Record
Identification
Creation 16.04.2009
Last edited 02.10.2017
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