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.
Peptidomimetics containing a vinyl ketone warhead as falcipain-2 inhibitors / R. Ettari, M. Zappalà, N. Micale, G. Grazioso, S. Giofrè, T. Schirmeister, S. Grasso. - In: EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY. - ISSN 0223-5234. - 46:6(2011), pp. 2058-2065. [10.1016/j.ejmech.2011.02.058]
Peptidomimetics containing a vinyl ketone warhead as falcipain-2 inhibitors
G. Grazioso;
2011
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.
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