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Literature DB >> 16722625

Novel peptidomimetic cysteine protease inhibitors as potential antimalarial agents.

Nicola Micale¹, Alan P Kozikowski, Roberta Ettari, Silvana Grasso, Maria Zappalà, Jong-Jin Jeong, Ajay Kumar, Manjit Hanspal, Athar H Chishti.

Abstract

The synthesis of a new class of peptidomimetics 1a-j, based on a 1,4-benzodiazepine scaffold and on a C-terminal aspartyl aldehyde building block, is described. Compounds 1a-j provided significant inhibitory activity against falcipains 2A and 2B (FP-2A and FP-2B), two cysteine proteases from Plasmodium falciparum.

Entities: Chemical Species

Mesh：

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Year: 2006 PMID： 16722625 DOI： 10.1021/jm060405f

Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446

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Cited

9 in total

1. Inhibition of Plasmodium falciparum oocyst production by membrane-permeant cysteine protease inhibitor E64d.

Authors: S Eksi; B Czesny; G-J van Gemert; R W Sauerwein; W Eling; K C Williamson
Journal: Antimicrob Agents Chemother Date: 2006-12-18 Impact factor: 5.191

2. Copper-catalyzed ligand-free amidation of aryl iodides and amino acid amides to synthesize C3-(Z)-1H-benzo[e][1,4]diazepin-2(3H)-ones.

Authors: Xiao Hu; Yi Dong; Gang Liu
Journal: Mol Divers Date: 2015-06-07 Impact factor: 2.943

3. Novel anti-plasmodial hits identified by virtual screening of the ZINC database.

Authors: Grace Mugumbate; Ana S Newton; Philip J Rosenthal; Jiri Gut; Rui Moreira; Kelly Chibale; Rita C Guedes
Journal: J Comput Aided Mol Des Date: 2013-10-25 Impact factor: 3.686

4. Plasmodium yoelii inhibitor of cysteine proteases is exported to exomembrane structures and interacts with yoelipain-2 during asexual blood-stage development.

Authors: Ying Pei; Jessica L Miller; Scott E Lindner; Ashley M Vaughan; Motomi Torii; Stefan H I Kappe
Journal: Cell Microbiol Date: 2013-03-14 Impact factor: 3.715

9. Identification of Tight-Binding Plasmepsin II and Falcipain 2 Inhibitors in Aqueous Extracts of Marine Invertebrates by the Combination of Enzymatic and Interaction-Based Assays.

Authors: Emir Salas-Sarduy; Yasel Guerra; Giovanni Covaleda Cortés; Francesc Xavier Avilés; María A Chávez Planes
Journal: Mar Drugs Date: 2017-04-21 Impact factor: 5.118

9 in total

Novel peptidomimetic cysteine protease inhibitors as potential antimalarial agents.

1. Inhibition of Plasmodium falciparum oocyst production by membrane-permeant cysteine protease inhibitor E64d.

2. Copper-catalyzed ligand-free amidation of aryl iodides and amino acid amides to synthesize C3-(Z)-1H-benzo[e][1,4]diazepin-2(3H)-ones.

3. Novel anti-plasmodial hits identified by virtual screening of the ZINC database.

4. Plasmodium yoelii inhibitor of cysteine proteases is exported to exomembrane structures and interacts with yoelipain-2 during asexual blood-stage development.

5. Antimalarial activity of thiosemicarbazones and purine derived nitriles.

6. BDA-410: a novel synthetic calpain inhibitor active against blood stage malaria.

Review 7. Isocyanide-based multicomponent reactions towards cyclic constrained peptidomimetics.

8. In silico Guided Drug Repurposing: Discovery of New Competitive and Non-competitive Inhibitors of Falcipain-2.

9. Identification of Tight-Binding Plasmepsin II and Falcipain 2 Inhibitors in Aqueous Extracts of Marine Invertebrates by the Combination of Enzymatic and Interaction-Based Assays.