Synthesis and antitumor activity of pefloxacin C-3 (rhodanine unsaturated ketone) amide derivatives / 中国药科大学学报

To explore a new strategy for the transformation of antibacterial activity of fluoroquinolone into antitumor activity,twelve new title compounds,1-ethyl-6-fluoro-7-(4-methyl-pipreazin-1-yl)-quinolin-4-one-3-carboxylicacid (5-arylidene-2-thioxo-1,3-thiozolidin-2,4-dione-3-yl) amides (6a-61),were designed and synthesized with an amide group and a rhodanine unsaturated ketone moiety as an isostere and modified group,respectively,from pefloxacin (1).Their structures were characterized by elemental analysis and spectral data.The in vitro antitumor activity of the title compounds against Hep-3B,Capan-1 and L1210 cell lines exhibited more significant potency than pefloxacin.The compounds with aromatic heterocyclic or flurophenyl displayed comparable activity to the comparasion doxorubicin.Thus,rhodanine unsaturated ketone hybrided amide group as an isostere of the C-3 carboxylic acid group appears to be an alternative route for further design of antitumor fluoroquinolone.

Curative effect observation and relative nursing of Nd∶YAG laser assisting the drug treatment for the patients with recurrent oral ulcer / 现代临床护理

Objective To explore the curative effect and relative nursing care key points of Nd∶YAG laser assisting the drug treatment for patients with recurrent oral ulcer.Methods Toally 82 patients with recurrent oral ulcer treated in our department were selected and alternately divided into experiment group (41 cases) and control group (41 cases) according to the initial visiting sequence with same gender.The control group used the conventional drug treatment.On the basis of conventional drug treatment,the experiment group additionally used the Nd∶YAG laser radiation therapy.The curative effects of both groups were evaluated after relative treatment for 4 days.Results The total effective rates of curative effects of two groups had significantly statistical differences (P＜0.001).The total effective rate of the experiment group was,significantly higher than that of the control group.Conclusions Nd∶YAG laser assisting the drug treatment for the patients with recurrent oral ulcer can significantly increase the total effective rate.The correct nursing services throughout the operative process are the important guarantee of good curative effect.