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Title
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Selection of a respiratory syncytial virus fusion inhibitor clinical candidate: 2: discovery of a morpholinopropylaminobenzimidazole derivative (TMC353121)
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Author
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Abstract
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| 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. |
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Language
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English
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Source (journal)
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Journal of medicinal chemistry. - Washington, D.C., 1963, currens
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Publication
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Washington, D.C.
:
2008
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ISSN
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0022-2623
[print]
1520-4804
[online]
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DOI
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10.1021/JM701284J
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Volume/pages
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51
:4
(2008)
, p. 875-896
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ISI
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000253353800019
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Full text (Publisher's DOI)
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