新型2-(1-(2-(取代苯基)-5-甲基恶唑-4-基)-3-(2-取代苯基)-4,5-二氢-1H-吡唑-5-基)-7-取代-1,2,3,4-四氢异喹啉衍生物的合成、结构及抗菌活性
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.
作者信息
Liu Xin-Hua, Zhu Jing, Zhou An-na, Song Bao-An, Zhu Hai-Liang, Bai Lin-Shan, Bhadury Pinaki S, Pan Chun-Xiu
机构信息
School of Chemistry and Chemical Engineering, Anhui Key Laboratory of Coal Clean Conversion and Utilization, Anhui University of Technology, Maanshan 243002, PR China.
出版信息
Bioorg Med Chem. 2009 Feb 1;17(3):1207-13. doi: 10.1016/j.bmc.2008.12.034. Epub 2008 Dec 24.
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 IC(50s) of 0.125 and 0.25 microg/mL against S. aureus DNA gyrase, 0.25 and 0.125 microg/mL against B. subtilis DNA gyrase). On the basis of the biological results, structure-activity relationships were also discussed.
合成了一系列新型的2-(1-(2-(取代苯基)-5-甲基恶唑-4-基)-3-(2-取代苯基)-4,5-二氢-1H-吡唑-5-基)-7-取代-1,2,3,4-四氢异喹啉衍生物。结果表明，化合物9q和10q能强烈抑制金黄色葡萄球菌DNA促旋酶和枯草芽孢杆菌DNA促旋酶（对金黄色葡萄球菌DNA促旋酶的IC50分别为0.125和0.25μg/mL，对枯草芽孢杆菌DNA促旋酶的IC50分别为0.25和0.125μg/mL）。基于生物学结果，还讨论了构效关系。
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