69504-29-6Relevant articles and documents
Fragment-based design, docking, synthesis, biological evaluation and structure-activity relationships of 2-benzo/benzisothiazolimino-5-aryliden-4- thiazolidinones as cycloxygenase/lipoxygenase inhibitors
Eleftheriou, Phaedra,Geronikaki, Athina,Hadjipavlou-Litina, Dimitra,Vicini, Paola,Filz, Olga,Filimonov, Dmitry,Poroikov, Vladimir,Chaudhaery, Shailendra S.,Roy, Kuldeep K.,Saxena, Anil K.
scheme or table, p. 111 - 124 (2012/03/09)
Balanced modulation of several targets is one of the current strategies for the treatment of multi-factorial diseases. Based on the knowledge of inflammation mechanisms, it was inferred that the balanced inhibition of cyclooxygenase-1/cyclooxygenase-2/lip
2-Heteroarylimino-5-benzylidene-4-thiazolidinones analogues of 2-thiazolylimino-5-benzylidene-4-thiazolidinones with antimicrobial activity: Synthesis and structure-activity relationship
Vicini, Paola,Geronikaki, Athina,Incerti, Matteo,Zani, Franca,Dearden, John,Hewitt, Mark
, p. 3714 - 3724 (2008/12/21)
2-Heteroarylimino-5-benzylidene-4-thiazolidinones, unsubstituted or carrying hydroxy, methoxy, nitro and chloro groups on the benzene ring, were synthesised and assayed in vitro for their antimicrobial activity against Gram positive and Gram negative bacteria, yeasts and mould. The antimicrobial activity of the 2-benzo[d]thiazolyl- and of the 2-benzo[d]isothiazolyl-imino-5-benzylidene-4-thiazolidinones is, on the whole, lower in comparison with the high activity detected for the derivatives of the 2-thiazolylimino-5-benzylidene-4-thiazolidinone class. Nevertheless most of the benzo[d]thiazole analogues display good inhibition of the growth of Gram positive bacilli and staphylococci, including methicillin-resistant Staphylococcus strains. Among the 2-benzo[d]isothiazole analogues a few derivatives show a strong and selective activity against bacilli. Moreover, it is worth noting that the replacement of the thiazole nucleus for the benzo[d]thiazole bicyclic system in the parent 2-(benzo[d]thiazol-2-ylimino)thiazolidin-4-one leads to significant antifungal properties against both yeasts and moulds, properties not shown by the analogous 2-thiazolyl- and 2-benzo[d]isothiazolyl-imino)thiazolidin-4-ones. The structure-activity relationship of 33 analogues possessing the 2-heteroarylimino-4-thiazolidinone structure is analysed through QSAR models.
Synthesis and local anesthetic activity of alkylaminoacyl derivatives of 3-amino-1,2-benzisothiazoles
Vicini,Amoretti,Chiavarini,Impicciatore
, p. 933 - 943 (2007/10/02)
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