Synthesis of novel peptidomimetics as inhibitors of protozoan cysteine proteases falcipain-2 and rhodesain
| Autor: | Roberta Ettari, Silvana Grasso, Matthias Leippe, Astrid Evers, Nicola Micale, Christoph Gelhaus, Maria Zappalà, Tanja Schirmeister |
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| Rok vydání: | 2010 |
| Předmět: |
Pharmacology
Proteases Peptidomimetic Chemistry Stereochemistry Plasmodium falciparum Organic Chemistry General Medicine Peptidomimetics Falcipain-2 inhibitors Rhodesain inhibitors Cysteine proteases Combinatorial chemistry Substrate Specificity Cysteine Endopeptidases Inhibitory Concentration 50 Drug Discovery Humans Protease Inhibitors Peptides Trypanocidal agent Cysteine |
| Zdroj: | European Journal of Medicinal Chemistry. 45:3228-3233 |
| ISSN: | 0223-5234 |
| Popis: | This paper describes the synthesis of novel peptidomimetics bearing a protected aspartyl aldeyde warhead leading to the thioacylals 2a,b and the acylals 3a,b. Compounds 2a and 3a proved to possess an increased antiplasmodial activity with respect to the parent molecule 1. Furthermore thioacylal 2a can be considered as a promising trypanocidal agent. |
| Databáze: | OpenAIRE |
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