Synthesis,structure and antibacterial activity of new 2-(1-(2-(substituted-phenyl)-5-methyloxazol-4-yl)-3-(2-substitued-phenyl)-4,5-dihydro-1H-pyrazol-5-yl)-7-substitued-1,2,3,4-tetrahydroisoquinoline derivatives |
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| Authors: | Xin-Hua Liu Jing Zhu An-na Zhou Bao-An Song Hai-Liang Zhu Lin-Shan bai Pinaki S Bhadury Chun-Xiu Pan |
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| Institution: | 1. School of Chemistry and Chemical Engineering, Anhui Key Laboratory of Coal Clean Conversion and Utilization, Anhui University of Technology, Maanshan 243002, PR China;2. Key Laboratory of Green Pesticide and Agriculture Bioengineering, Ministry of Education, Guizhou University, Guiyang 550025, PR China;3. State Key Laboratory of Pharmaceutical Biotechnology, Nanjing University, Nanjing 210093, PR China |
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| Abstract: | A series of new 2-(1-(2-(substituted-phenyl)-5-methyloxazol-4-yl)-3-(2-substitued-phenyl)-4,5-dihydro-1H-pyrazol-5-yl)-7-substitued-1,2,3,4-tetrahydroisoquinoline derivatives were synthesized. The results showed that compounds 9q and 10q can strongly inhibit Staphylococcus aureus DNA gyrase and Bacillus subtilis DNA gyrase (with IC50s of 0.125 and 0.25 μg/mL against S. aureus DNA gyrase, 0.25 and 0.125 μg/mL against B. subtilis DNA gyrase). On the basis of the biological results, structure–activity relationships were also discussed. |
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