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Peptidomimetics containing a vinyl ketone warhead as falcipain-2 inhibitors
- Source :
-
European Journal of Medicinal Chemistry . Jun2011, Vol. 46 Issue 6, p2058-2065. 8p. - Publication Year :
- 2011
-
Abstract
- Abstract: The design, chemical synthesis, and enzymatic activity evaluation of a set of falcipain-2 inhibitors are reported. These compounds contain a proven peptidomimetic recognition motif based on a benzo[1,4]diazepin-2-one (1,4-BDZ) framework built on a dipeptide sequence, and a Michael acceptor terminal moiety capable of deactivating the cysteine protease active site. Our goal is to modify the P3 site of this motif in order to identify the structural requirements for the interaction with the target. [Copyright &y& Elsevier]
Details
- Language :
- English
- ISSN :
- 02235234
- Volume :
- 46
- Issue :
- 6
- Database :
- Academic Search Index
- Journal :
- European Journal of Medicinal Chemistry
- Publication Type :
- Academic Journal
- Accession number :
- 60378334
- Full Text :
- https://doi.org/10.1016/j.ejmech.2011.02.058