A series of novel calix[4]arene derivatives incorporating two triazolyl 1 3-diketo subunits in alternate positions at the lower rim were synthesized and screened for HⅣ integrase inhibition activity.The chemical structures of these compounds were confirmed by means of1H NMR 13C NMR,and ESI-MS.Preliminary bioassays indicated that calix[4]arene derivatives proved to be more active than p-tertbutylcalix[4]arene derivatives.In particular,compound 4g presented the most potent integrase strand transfer inhibitory activity with an IC50value of 6.1 mmol/L.
Zai-Gang LuoYu ZhaoChao MaXue-Mei XuXiao-Mei ZhangNian-Yu HuangHong-Qiu He
To quantitatively determine tylosin and tilmicosin in edible animal tissues,a time-resolved fluoroimmunoassay(TRFIA) has been developed and validated.For this purpose,desmycosin-O-carboxymethoxylamine-BSA was fixed onto microtiter plates,standards and samples were loaded and,finally,diluted europium-labeled anti-tylosin antibodies were added.Results show that the limit of detection for tylosin was 0.03 ng mL-1 and that for tilmicosin was 0.05 ng mL-1.The recoveries were 73.6% to 120.5%,with coefficients of variation below 15.6% in various biological matrices spiked with tylosin and tilmicosin at concentrations of 50-200 ngg-1.There was good correlation(R2>0.99) between the TRFIA,an enzyme-linked immunosorbent assay and high performance liquid chromatography data.In conclusion,the new TRFIA is applicable to the detection of tylosin and tilmicosin and is an effective and economical method that will enable high-throughput sample screening.The method is expected to be widely applicable.
WEI ShuLE TaoCHEN YongXU JianHE HongQiuNIU XiaoDongLUO JinHua
