Synthesis of 2-Hydrazolyl-4-Thiazolidinones Based on Multicomponent Reactions and Biological Evaluation Against Trypanosoma Cruzi

A series of 18 novel 2-hydrazolyl-4-thiazolidinones-5-carboxylic acids, amides and 5,6-α,β-unsaturated esters were synthesized, and their in vitro activity on cruzipain and T. cruzi epimastigotes was determined. Some agents show activity at 37 μm concentration in the enzyme assay. Computational tool...

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Veröffentlicht in:	Chemical biology & drug design 2011-03, Vol.77 (3), p.166-172
Hauptverfasser:	Pizzo, Chiara, Saiz, Cecilia, Talevi, Alan, Gavernet, Luciana, Palestro, Pablo, Bellera, Carolina, Blanch, Luis Bruno, Benítez, Diego, Cazzulo, Juan J, Chidichimo, Agustina, Wipf, Peter, Mahler, S. Graciela
Format:	Artikel
Sprache:	eng
Schlagworte:	2-hydrazolyl-4-thiazolidinone Acetamides - chemical synthesis Acetamides - chemistry Acetamides - toxicity Acids amides Animals Antiprotozoal Agents - chemical synthesis Antiprotozoal Agents - chemistry Antiprotozoal Agents - toxicity Binding Sites Catalytic Domain Cercopithecus aethiops Chagas disease Computer applications Computer Simulation cruzipain Cysteine Endopeptidases - chemistry Cysteine Endopeptidases - metabolism Drug development Enzymes Epimastigotes Esters inhibitors multicomponent connection reaction Quantitative Structure-Activity Relationship Thiazolidines - chemistry Trypanosoma cruzi Trypanosoma cruzi - drug effects Trypanosoma cruzi - enzymology Vero Cells
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