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.
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.
Liu
Xin-Hua
XH
School of Chemistry and Chemical Engineering, Anhui Key Laboratory of Coal Clean Conversion and Utilization, Anhui University of Technology, Maanshan 243002, PR China. xhliuhx@163.com
Zhu
Jing
J
Zhou
An-na
AN
Song
Bao-An
BA
Zhu
Hai-Liang
HL
Bai
Lin-Shan
LS
Bhadury
Pinaki S
PS
Pan
Chun-Xiu
CX
D000900:Anti-Bacterial Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D001412:Bacillus subtilis / Q000187:drug effects; D027081:DNA Gyrase / Q000378:metabolism; D020128:Inhibitory Concentration 50; D007546:Isoquinolines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D008826:Microbial Sensitivity Tests; D013211:Staphylococcus aureus / Q000187:drug effects; D059005:Topoisomerase II Inhibitors
D000900:Anti-Bacterial Agents; D007546:Isoquinolines; D059005:Topoisomerase II Inhibitors; D027081:DNA Gyrase