eprintid: 18773
rev_number: 12
userid: 1419
dir: disk0/00/01/87/73
datestamp: 2013-05-28 15:38:04
lastmod: 2017-10-28 13:55:13
status_changed: 2013-05-28 15:38:04
type: article
metadata_visibility: show
item_issues_count: 0
eprint_status: archive
creators_name: Pizzo, C
creators_name: Saiz, C
creators_name: Talevi, A
creators_name: Gavernet, L
creators_name: Palestro, P
creators_name: Bellera, C
creators_name: Blanch, LB
creators_name: Benítez, D
creators_name: Cazzulo, JJ
creators_name: Chidichimo, A
creators_name: Wipf, P
creators_name: Mahler, SG
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creators_email: pwipf@pitt.edu
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creators_id: PWIPF
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title: Synthesis of 2-Hydrazolyl-4-Thiazolidinones Based on Multicomponent Reactions and Biological Evaluation Against Trypanosoma Cruzi
ispublished: pub
divisions: sch_as_chemistry
full_text_status: public
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.
date: 2011-03-01
date_type: published
publication: Chemical Biology and Drug Design
volume: 77
number: 3
pagerange: 166 - 172
refereed: TRUE
issn: 1747-0277
id_number: 10.1111/j.1747-0285.2010.01071.x
pmid: 21251233
mesh_headings: Acetamides--chemical synthesis
mesh_headings: Acetamides--chemistry
mesh_headings: Acetamides--toxicity
mesh_headings: Animals
mesh_headings: Antiprotozoal Agents--chemical synthesis
mesh_headings: Antiprotozoal Agents--chemistry
mesh_headings: Antiprotozoal Agents--toxicity
mesh_headings: Binding Sites
mesh_headings: Catalytic Domain
mesh_headings: Cercopithecus aethiops
mesh_headings: Computer Simulation
mesh_headings: Cysteine Endopeptidases--chemistry
mesh_headings: Cysteine Endopeptidases--metabolism
mesh_headings: Quantitative Structure-Activity Relationship
mesh_headings: Thiazolidines--chemistry
mesh_headings: Trypanosoma cruzi--drug effects
mesh_headings: Trypanosoma cruzi--enzymology
mesh_headings: Vero Cells
chemical_names: Acetamides
chemical_names: Antiprotozoal Agents
chemical_names: Thiazolidines
chemical_names: acetamide
chemical_names: Cysteine Endopeptidases
chemical_names: cruzipain
citation:   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     
document_url: http://d-scholarship-dev.library.pitt.edu/18773/1/licence.txt