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Mini-Reviews in Medicinal Chemistry
ISSN (Print): 1389-5575
ISSN (Online): 1875-5607
Epub Abstract Ahead of Print
DOI: 10.2174/13895575113139990004      Price:  $95

Pharmacological activities on thiazolidine-4-carboxylic acid and derivatives containing thiazolyl group

Author(s): Zhong-Cheng Song and Hai-Liang Zhu
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Five members ring thiazole or thizolidine presents in many interesting compounds as well as the aryl- and hetero- rings. The compounds containing thiazole or thizolidine nucleus, especially containing skeleton thiazolidine-4-carboxylic acid and its’ derivatives were separated from natural products or synthesized in the lab. The importance appears to have grown over the years, because it was tested that these compounds displayed different pharmaceutical activities. Regarding other thiazolidine-4-carboxylic acid derivatives, main activities have been claimed in most of compounds such as peroxisome proliferating-activated receptor  (PPAR) agonist, inhibition of enzyme, antagonist, antibacterial activity, inhibitory activity against aldose reductase, hepatoprotective activity, inhibition of fibril formation, activity against acetaminophen-induced hepatotoxicity, increase of cytotoxicity, pharmacokinetics effect, antiviral activity, anti HIV activity, antioxidant activity, immunostimulatory activity, vasorelaxing effect, anti-tumor activity, protection from acetaminophen-induced liver necrosis, cytotoxic activity, inhibition of inositol requiring enzyme 1α. Few compounds were founded some especial activities, for example: inhibition of 2,2-diphenyl-1-picryl-hydrazyl (DPPH)-induced radical production, inhibition of FeII-induced radical production, radioprotective activity, cataract development prevention, binding to auxin receptor TIR1, neurotrophic activity, et al. Moreover, some derivatives containing thiazolyl group exhibited FabH inhibitory activities, EGFR kinase inhibitory activities, FAK inhibitory activities, telomerase inhibitory activities, antiproliferaction activities against MCF and A549, COX-2 inhibitor, and so on. This review is based on the fact that the basic skeleton thiazolidine-4-carboxylic acid and thizolyl group are present in many chemically interesting compounds that display biological activities.
College of Bioengineering, Zhejiang Chinese Medical University, Hangzhou 310053, P. R. China