title: 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.
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 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.
authors.affiliation: 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
authors.forename: Xin-Hua
authors.initials: XH
authors.lastname: Liu
authors.forename: Jing
authors.initials: J
authors.lastname: Zhu
authors.forename: An-na
authors.initials: AN
authors.lastname: Zhou
authors.forename: Bao-An
authors.initials: BA
authors.lastname: Song
authors.forename: Hai-Liang
authors.initials: HL
authors.lastname: Zhu
authors.forename: Lin-Shan
authors.initials: LS
authors.lastname: Bai
authors.forename: Pinaki S
authors.initials: PS
authors.lastname: Bhadury
authors.forename: Chun-Xiu
authors.initials: CX
authors.lastname: Pan
mesh_terms: 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
chemical_list: D000900:Anti-Bacterial Agents; D007546:Isoquinolines; D059005:Topoisomerase II Inhibitors; D027081:DNA Gyrase