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

被引：25

作者：

Modric, Marina ^{[1
]}

Bozicevic, Marin ^{[2
]}

Faraho, Ivan ^{[3
]}

Bosnar, Martina ^{[3
]}

Skoric, Irena ^{[2
]}

机构：

[1] Fidelta Ltd, Chem, Prilaz Baruna Filipovica 20, HR-10000 Zagreb, Croatia

[2] Univ Zagreb, Fac Chem Engn & Technol, Dept Organ Chem, Marulicev Trg 19, HR-10000 Zagreb, Croatia

[3] Fidelta Ltd, Pharmacol Vitro, Prilaz Baruna Filipovica 29, HR-10000 Zagreb, Croatia

来源：

JOURNAL OF MOLECULAR STRUCTURE | 2021年 / 1239卷

关键词：

Thiazole; Small chemical fragments; Library design; Anti-inflammatory activity; DISCOVERY; THIAZOLE;

D O I：

10.1016/j.molstruc.2021.130526

中图分类号：

O64 [物理化学（理论化学）、化学物理学];

学科分类号：

070304 ; 081704 ;

摘要：

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 TNF alpha and IL-8 release with IC50 values in mu M range without cytotoxic activity. (C) 2021 Elsevier B.V. All rights reserved.

引用

页数：12

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