Antitubercular properties of thiazolidin-4-ones - A review
| Autor: | Nazar Trotsko |
|---|---|
| Rok vydání: | 2020 |
| Předmět: |
THP-1 Cells
Antitubercular Agents Microbial Sensitivity Tests 01 natural sciences Mycobacterium 03 medical and health sciences Structure-Activity Relationship Drug Discovery Chlorocebus aethiops Animals Humans Vero Cells 030304 developmental biology Thiazolidine 2 4 dione Pharmacology 0303 health sciences Molecular Structure 010405 organic chemistry Chemistry Organic Chemistry Acidomycin Biological activity General Medicine Combinatorial chemistry Small molecule 0104 chemical sciences Mic values Molecular targets Thiazolidines |
| Zdroj: | European journal of medicinal chemistry. 215 |
| ISSN: | 1768-3254 |
| Popis: | Thiazolidin-4-one scaffold has great potential for medicinal chemistry and is of interest to scientists in view of wide spectrum of biological activity. This scaffold is often used for designing of small molecules with various biological activity including antituberculosis activity. The presented review is an attempt to gather, analyze and systemize data about antitubercular properties of thiazolidine-4-ones from two last decades. Some of them have promising antitubercular activity which is significantly higher than that of the reference drugs. Among them compounds 82c, 82d and 84 that were active against M. tuberculosis H37Rv strain with MICs in the range of 0.05–0.2 μg/mL and compound 108 exhibited activity with MIC = 0.36 μM. Compounds 115a-115c and 116a-116c were very effective against M. tuberculosis H37Ra with MIC values in the range of 0.031–0.125 μg/mL. Acidomycin was showed activity against seven MDR M. tuberculosis strains with MICs in the range of 0.6–0.62 μM and against two XDR M. tuberculosis strains with MICs 0.096 and 1.2 μM. The structure-activity relationship (SAR) of some groups of compounds, as well as some potential molecular targets were also discussed. |
| Databáze: | OpenAIRE |
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