BIOMAT Database Logo BIOMAT Database Logo

Design, synthesis and biological evaluation of metronidazole-thiazole derivatives as antibacterial inhibitors. 2014

Ya-Juan Qin, and Peng-Fei Wang, and Jigar A Makawana, and Zhong-Chang Wang, and Ze-Nan Wang, and Yan-Gu, and Ai-Qin Jiang, and Hai-Liang Zhu
State Key Laboratory of Pharmaceutical Biotechnology, School of Life Science Nanjing University, Nanjing 210093, People's Republic of China.

A series of metronidazole-thiazole derivatives has been designed, synthesized and evaluated as potential antibacterial inhibitors. All the synthesized compounds were determined by elemental analysis, 1H NMR and MS. They were also tested for antibacterial activity against Escherichia coli, Bacillus thuringiensis, Bacillus subtilis and Pseudomonas aeruginosa as well as for the inhibition to FabH. The results showed that compound 5e exhibited the most potent inhibitory activity against E. coli FabH with IC50 of 4.9μM. Molecular modeling simulation studies were performed in order to predict the biological activity of proposed compounds. Toxicity assay of compounds 5a, 5b, 5d, 5e, 5g and 5i showed that they were noncytotoxic against human macrophage. The results revealed that these compounds offered remarkable viability.

UI MeSH Term Description Entries

Related Publications

Ya-Juan Qin, and Peng-Fei Wang, and Jigar A Makawana, and Zhong-Chang Wang, and Ze-Nan Wang, and Yan-Gu, and Ai-Qin Jiang, and Hai-Liang Zhu
Design, synthesis and biological evaluation of novel thiazole derivatives as potent FabH inhibitors.
December 2009, Bioorganic & medicinal chemistry letters,
Ya-Juan Qin, and Peng-Fei Wang, and Jigar A Makawana, and Zhong-Chang Wang, and Ze-Nan Wang, and Yan-Gu, and Ai-Qin Jiang, and Hai-Liang Zhu
Synthesis and biological evaluation of thiazole derivatives as LbSOD inhibitors.
December 2019, Journal of enzyme inhibition and medicinal chemistry,
Ya-Juan Qin, and Peng-Fei Wang, and Jigar A Makawana, and Zhong-Chang Wang, and Ze-Nan Wang, and Yan-Gu, and Ai-Qin Jiang, and Hai-Liang Zhu
Design, synthesis and biological evaluation of novel thiazole-based derivatives as human Pin1 inhibitors.
January 2021, Bioorganic & medicinal chemistry,
Ya-Juan Qin, and Peng-Fei Wang, and Jigar A Makawana, and Zhong-Chang Wang, and Ze-Nan Wang, and Yan-Gu, and Ai-Qin Jiang, and Hai-Liang Zhu
Design, synthesis and biological evaluation of novel coumarin thiazole derivatives as α-glucosidase inhibitors.
April 2016, Bioorganic chemistry,
Ya-Juan Qin, and Peng-Fei Wang, and Jigar A Makawana, and Zhong-Chang Wang, and Ze-Nan Wang, and Yan-Gu, and Ai-Qin Jiang, and Hai-Liang Zhu
Design and synthesis of thiazole derivatives as potent FabH inhibitors with antibacterial activity.
March 2014, European journal of medicinal chemistry,
Ya-Juan Qin, and Peng-Fei Wang, and Jigar A Makawana, and Zhong-Chang Wang, and Ze-Nan Wang, and Yan-Gu, and Ai-Qin Jiang, and Hai-Liang Zhu
Design, synthesis, molecular docking studies and biological evaluation of thiazole carboxamide derivatives as COX inhibitors.
March 2023, BMC chemistry,
Ya-Juan Qin, and Peng-Fei Wang, and Jigar A Makawana, and Zhong-Chang Wang, and Ze-Nan Wang, and Yan-Gu, and Ai-Qin Jiang, and Hai-Liang Zhu
Design, synthesis, docking and biological evaluation of 4-phenyl-thiazole derivatives as autotaxin (ATX) inhibitors.
September 2017, Bioorganic & medicinal chemistry letters,
Ya-Juan Qin, and Peng-Fei Wang, and Jigar A Makawana, and Zhong-Chang Wang, and Ze-Nan Wang, and Yan-Gu, and Ai-Qin Jiang, and Hai-Liang Zhu
Synthesis and biological evaluation of thiazole derivatives as novel USP7 inhibitors.
February 2017, Bioorganic & medicinal chemistry letters,
Ya-Juan Qin, and Peng-Fei Wang, and Jigar A Makawana, and Zhong-Chang Wang, and Ze-Nan Wang, and Yan-Gu, and Ai-Qin Jiang, and Hai-Liang Zhu
Design, synthesis and biological evaluation of novel thiazole-derivatives as mitochondrial targeting inhibitors of cancer cells.
September 2021, Bioorganic chemistry,
Ya-Juan Qin, and Peng-Fei Wang, and Jigar A Makawana, and Zhong-Chang Wang, and Ze-Nan Wang, and Yan-Gu, and Ai-Qin Jiang, and Hai-Liang Zhu
Design, synthesis and biological evaluation of indeno[1,2-d]thiazole derivatives as potent histone deacetylase inhibitors.
June 2013, Bioorganic & medicinal chemistry letters,
Copied contents to your clipboard!