Constrained peptidomimetics as antiplasmodial falcipain-2 inhibitors

被引：34

作者：

Bova, Floriana ^{[1
]}

Ettari, Roberta ^{[1
]}

Micale, Nicola ^{[1
]}

Carnovale, Caterina ^{[1
]}

Schirmeister, Tanja ^{[2
]}

Gelhaus, Christoph ^{[3
]}

Leippe, Matthias ^{[3
]}

Grasso, Silvana ^{[1
]}

Zappala, Maria ^{[1
]}

机构：

[1] Univ Messina, Dipartimento Farmacochim, I-98168 Messina, Italy

[2] Univ Wurzburg, Inst Pharm & Food Chem, D-97074 Wurzburg, Germany

[3] Univ Kiel, Inst Zool, D-24098 Kiel, Germany

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2010年 / 18卷 / 14期

关键词：

Peptidomimetics; Falcipain-2; inhibitors; Rhodesain inhibitors; Cysteine proteases; CYSTEINE PROTEASE; PLASMODIUM-FALCIPARUM; RECOMBINANT FALCIPAIN-2; VINYL; SUBSTRATE; EFFICIENT;

D O I：

10.1016/j.bmc.2010.06.010

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

Herein we report the synthesis of a series of novel constrained peptidomimetics 2-10 endowed with a dipeptide backbone (D-Ser-Gly) and a vinyl ester warhead, structurally related to a previously identified lead compound 1, an irreversible inhibitor of falcipain-2, the main haemoglobinase of lethal malaria parasite Plasmodium falciparum. The new compounds were evaluated for their inhibition against falcipain-2, as well as against cultured P. falciparum. The inhibitory activity of the synthesized compounds was also evaluated against another protozoal cysteine protease, namely rhodesain of Trypanosoma brucei rhodesiense. (C) 2010 Elsevier Ltd. All rights reserved.

引用

页码：4928 / 4938

页数：11

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