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

Pizzo, C and Saiz, C and Talevi, A and Gavernet, L and Palestro, P and Bellera, C and Blanch, LB and Benítez, D and Cazzulo, JJ and Chidichimo, A and Wipf, P and Mahler, SG (2011) Synthesis of 2-Hydrazolyl-4-Thiazolidinones Based on Multicomponent Reactions and Biological Evaluation Against Trypanosoma Cruzi. Chemical Biology and Drug Design, 77 (3). 166 - 172. ISSN 1747-0277

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Abstract

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 37μm concentration in the enzyme assay. Computational tools and docking were used to correlate the biological response with the physicochemical parameters of the compounds and their cruzipain inhibitory effects. © 2011 John Wiley & Sons A/S.


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Details

Item Type: Article
Status: Published
Creators/Authors:
CreatorsEmailPitt UsernameORCID
Pizzo, C
Saiz, C
Talevi, A
Gavernet, L
Palestro, P
Bellera, C
Blanch, LB
Benítez, D
Cazzulo, JJ
Chidichimo, A
Wipf, Ppwipf@pitt.eduPWIPF
Mahler, SG
Date: 1 March 2011
Date Type: Publication
Journal or Publication Title: Chemical Biology and Drug Design
Volume: 77
Number: 3
Page Range: 166 - 172
DOI or Unique Handle: 10.1111/j.1747-0285.2010.01071.x
Schools and Programs: Dietrich School of Arts and Sciences > Chemistry
Refereed: Yes
ISSN: 1747-0277
MeSH Headings: Acetamides--chemical synthesis; Acetamides--chemistry; Acetamides--toxicity; Animals; Antiprotozoal Agents--chemical synthesis; Antiprotozoal Agents--chemistry; Antiprotozoal Agents--toxicity; Binding Sites; Catalytic Domain; Cercopithecus aethiops; Computer Simulation; Cysteine Endopeptidases--chemistry; Cysteine Endopeptidases--metabolism; Quantitative Structure-Activity Relationship; Thiazolidines--chemistry; Trypanosoma cruzi--drug effects; Trypanosoma cruzi--enzymology; Vero Cells
PubMed ID: 21251233
Date Deposited: 28 May 2013 15:38
Last Modified: 28 Oct 2017 13:55
URI: http://d-scholarship.pitt.edu/id/eprint/18773

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