2-Heteroarylimino-5-benzylidene-4-thiazolidinones analogues of 2-thiazolylimino-5-benzylidene-4-thiazolidinones with antimicrobial activity: synthesis and structure-activity relationship.

Vicini P; Geronikaki A; Incerti MZani FDearden JHewitt M

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2-Heteroarylimino-5-benzylidene-4-thiazolidinones analogues of 2-thiazolylimino-5-benzylidene-4-thiazolidinones with antimicrobial activity: synthesis and structure-activity relationship.

机译：2-Heteroarylimino-5-benzylidene-4-thiazolidinones analogues of 2-thiazolylimino-5-benzylidene-4-thiazolidinones with antimicrobial activity: synthesis and structure-activity relationship.

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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-benzodthiazolyl- and of the 2-benzodisothiazolyl-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 benzodthiazole analogues display good inhibition of the growth of gram positive bacilli and staphylococci, including methicillin-resistant Staphylococcus strains. Among the 2-benzodisothiazole 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 benzodthiazole bicyclic system in the parent 2-(benzodthiazol-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-benzodisothiazolyl-imino)thiazolidin-4-ones. The structure-activity relationship of 33 analogues possessing the 2-heteroarylimino-4-thiazolidinone structure is analysed through QSAR models.

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来源
《Bioorganic and medicinal chemistry》 |2008年第7期|3714-3724|共11页
作者
Vicini P; Geronikaki A; Incerti MZani FDearden JHewitt M;
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作者单位

Dipartimento Farmaceutico, Universita degli Studi di Parma, Viale G.P. Usberti 27/A, Parma 43100, Italy. paola.vicini@unipr.it;

ost.saga-med.ac.jp;

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正文语种英语
中图分类药学;生物化学;
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Anti-Bacterial Agents; Benzylidene Compounds; Drug Design; Microbial Viability; 苄烯化合物; 药物设计; 分子结构; 构效关系;

2-Heteroarylimino-5-benzylidene-4-thiazolidinones analogues of 2-thiazolylimino-5-benzylidene-4-thiazolidinones with antimicrobial activity: synthesis and structure-activity relationship.

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