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8. Synthesis and schistosomicidal activity of new substituted thioxo-imidazolidine compounds

Author

M C P A, Albuquerque, T G, Silva, M G R, Pitta, A C A, Silva, P G, Silva, E, Malagueño, J V, Santana, A G, Wanderley, M C A, Lima, S L, Galdino, J, Barbe, and I R, Pitta

Subjects
Male, Mice, Schistosomicides, Magnetic Resonance Spectroscopy, Animals, Female, Indicators and Reagents, Schistosoma mansoni, Crystallography, X-Ray, Imidazolidines
Abstract

Synthesis and physico-chemical properties of 3-benzyl-5-(4-fluoro-benzylidene)-1-methyl-2-thioxo-imidazolidin-4-ones, 5-benzylidene-3-(4-nitro-benzyl)-2-thioxo-imidazolidin-4-ones and 4-acridin-9-ylmethylene-1-benzyl-5-thioxo-imidazolidin-2-ones compounds are described. These thioxo-imidazolidine derivatives were prepared by alkylation and condensation with 4-fluoro-benzaldehyde or nucleophilic Michael addition with cyanoacrylates. The schistosomicidal activity of 3-benzyl-5-(4-fluoro-benzylidene)-1-methyl-2-thioxo-imidazolidin-4-one compounds was evaluated.

Published
2005

9. Synthesis and structural study of substituted thioxothiazolidinones and thioxoimidazolidinones

Author

A M C, Andrade, W T, Lima, M P A, Rocha, M C A, Lima, S L, Galdino, J M, Barbosa Filho, A J S, Góes, and I R, Pitta

Subjects
Thiazoles, Magnetic Resonance Spectroscopy, Alkylation, Chemical Phenomena, Chemistry, Physical, Imidazoles, Thiones, Indicators and Reagents
Abstract

A new set of derivative thioxothiazolidinones and thioxoimidazolidinones 3,5-dissubstituted has been synthesized with satisfactory yield from the condensation Knoevenagel type between benzaldéhydes and 4-thioxothiazolidin-2-one, 2-thioxothiazolidin-4-one and 1-méthyl-2-thioxoimidazolidin-4-one compounds following by N-alkylation with aryl or acyl halides. The physico-chemical properties of the 5-benzylidene-3-[2-(4-chlorophenyl)-2-oxoethyl]-2 (or 4)-thioxothiazolidin-4 (or 2)-ones and 5-benzylidene-1-methyl-2-thioxoimidazolidin-4-ones synthesized have been described.

Published
2003

10. Substituted thiazolidinediones and thio-imidazolidinones: synthesis, structural study and pharmacological activity

Author

J F, Albuquerque, A, Albuquerque, C C, Azevedo, F, Thomasson, L S, Galdino, J, Chantegrel, M T, Catanho, I R, Pitta, and C, Luu-Duc

Subjects
Blood Glucose, Analgesics, Mice, Structure-Activity Relationship, Thiazoles, Magnetic Resonance Spectroscopy, Alkylation, Imidazoles, Animals, Hypoglycemic Agents, Pain Measurement
Abstract

Synthesis and physico-chemical properties of six 3-(4-bromophenacyl)-5-arylidene-thiazolidine-2,4-diones and eight 3-(4-chlorobenzyl)-5-arylidene-4-thio-imidazolidine-2-ones are described. These products were synthesized by an aldolisation-crotonisation reaction from aromatic aldehydes and 3-substituted thiazolidine-2,4-diones or 4-thio-imidazolidine-2-ones. Hypoglycemic and peripheral antinociceptive activities were investigated for these compounds.

Published
1995

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