Design, synthesis and biological evaluation of new 1,3-thiazole derivatives as potential anti-inflammatory agents

•Twenty six thiazole derivatives were designed and synthesized as a starting hits to be developed in the drug like molecules•Their in vitro anti-inflammatory activities have been screened in two assays•Compounds were screened in in vitro cell viability assays to evaluate potential cytotoxicity•Some...

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Veröffentlicht in:Journal of molecular structure 2021-09, Vol.1239, p.130526, Article 130526
Hauptverfasser: Modrić, Marina, Božičević, Marin, Faraho, Ivan, Bosnar, Martina, Škorić, Irena
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Sprache:eng
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Zusammenfassung:•Twenty six thiazole derivatives were designed and synthesized as a starting hits to be developed in the drug like molecules•Their in vitro anti-inflammatory activities have been screened in two assays•Compounds were screened in in vitro cell viability assays to evaluate potential cytotoxicity•Some screened compounds were found to be potent in the series by inhibiting LPS-induced TNFα release with IC50 values in µM range•One compound was found to be potent by inhibiting LPS-induced IL-8 release with IC50 values in µM range Thiazoles are widely recognized as nuclei of great value for obtaining molecules with various biological activities, including analgesic, anti-inflammatory, anti-HIV, antidiabetic, antitumor and antimicrobial. A library of 26 thiazole derivatives as fragments were designed, synthesized and evaluated for their anti-inflammatory activities. Some screened compounds showed promising results and were found to be potent in the series by inhibiting LPS-induced TNFα and IL-8 release with IC50 values in µM range without cytotoxic activity. [Display omitted]
ISSN:0022-2860
1872-8014
DOI:10.1016/j.molstruc.2021.130526