Optimization Strategy of Novel Peptide-Based Michael Acceptors for the Treatment of Human African Trypanosomiasis

6533b859fe1ef96bd12b77b2

RESEARCH PRODUCT

Optimization Strategy of Novel Peptide-Based Michael Acceptors for the Treatment of Human African Trypanosomiasis

Tanja Schirmeister Santo Previti Giorgio Amendola Sandro Cosconati Roberta Ettari Annika Wagner Santina Maiorana Ute A. Hellmich Maria Zappalà

subject

Trypanosoma brucei rhodesiense Strong inhibitor Ketone Stereochemistry Protein Conformation Peptide 01 natural sciences 03 medical and health sciences Structure-Activity Relationship SUBSTRATE Drug Discovery medicine Humans African trypanosomiasis Sulfones BIOLOGICAL EVALUATION 030304 developmental biology WARHEAD chemistry.chemical_classification 0303 health sciences Molecular Structure Chemistry DERIVATIVES Trypanosoma brucei rhodesiense CYSTEINE PROTEASES RHODESAIN BIOLOGICAL EVALUATION CATHEPSIN-L INHIBITORS BRUCEI PEPTIDOMIMETICS FALCIPAIN-2 DERIVATIVES SUBSTRATE WARHEAD BRUCEI medicine.disease FALCIPAIN-2 Trypanocidal Agents 0104 chemical sciences 010404 medicinal & biomolecular chemistry Cysteine Endopeptidases Trypanosomiasis African CYSTEINE PROTEASES RHODESAIN CATHEPSIN-L Molecular Medicine INHIBITORS PEPTIDOMIMETICS

description

This paper describes an optimization strategy of the highly active vinyl ketone 3 which was recognized as a strong inhibitor of rhodesain of Trypanosoma brucei rhodesiense, endowed with a ksecond v...

year	journal	country	edition	language
2019-01-01

10.1021/acs.jmedchem.9b00908 http://hdl.handle.net/11570/3148075

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