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Peptidomimetics containing a vinyl ketone warhead as falcipain-2 inhibitors.

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 P(3) site of this motif in order to identify the structural requirements for the interaction with the target.

journal_name

Eur J Med Chem

journal_title

European journal of medicinal chemistry

authors

Ettari R,Zappalà M,Micale N,Grazioso G,Giofrè S,Schirmeister T,Grasso S

doi

10.1016/j.ejmech.2011.02.058

subject

Has Abstract

pub_date

2011-06-01 00:00:00

pages

2058-65

issue

6

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(11)00186-3

journal_volume

46

pub_type

杂志文章

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