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Novel, potent, and orally bioavailable phosphinic acid inhibitors of the hepatitis C virus NS3 protease
- Source :
-
Bioorganic & Medicinal Chemistry Letters . Jun2011, Vol. 21 Issue 12, p3568-3572. 5p. - Publication Year :
- 2011
-
Abstract
- Abstract: A potent and novel class of product-like inhibitors of the HCV NS3 protease was discovered by employing a phosphinic acid as a carboxylate isostere. The replicon activity and pharmacokinetic profile of this series of compounds was optimized by exploring the substitution of the phosphinic acid, as well as conformationally constraining these compounds through macrocyclization. The syntheses and preliminary biological evaluation of these phosphinic acids is described. [Copyright &y& Elsevier]
Details
- Language :
- English
- ISSN :
- 0960894X
- Volume :
- 21
- Issue :
- 12
- Database :
- Academic Search Index
- Journal :
- Bioorganic & Medicinal Chemistry Letters
- Publication Type :
- Academic Journal
- Accession number :
- 61173411
- Full Text :
- https://doi.org/10.1016/j.bmcl.2011.04.125