1.Study on the Bioequivalence of Domestic and Imported Fluvoxamin Maleate Tablets in Healthy Volunteers
China Pharmacy 2007;0(26):-
0.05). CONCLUSION: Domestic and imported fluvoxamin maleate tablets are bioequivalent.
2.THE CLINICAL APPLICATION OF THE MONOCLONAL ANTIBODIES TARGETED ANTI-CANCER DRUGS IN ZHONGSHAN HOSPITAL
Ruomei XIAO ; Chuxin LIAO ; Guifeng WANG
Modern Hospital 2015;(4):93-96
Objective To know the current situation of the Monoclonal antibodies target anticancer drugs by collecting and analyzing data,to provide reference for the clinical reasonable application .Methods We collected 310 cases used the antibodies target anticancer drugs in the hospital of ZhongShan , analyzed its clinical efficacy, and evaluated the drugs'efficacy combining the time be hospitalized .Results The sum and number of charges of the Monoclonal antibodies targeted anticancer drugs are 13.67 percent and 0.12 percent in the total charges of anticancer drugs.There are 241 cases (78%) hospitalized in a single course of treatment within 14 days; 298(96%) comple-ted the chemotherapy successfully .Conclusion The monoclonal antibodies targeting anticancer drugs has the good clinical efficacy, and most of the adverse reactions are mild or moderate which can recover after treated .The key fac-tor limited the clinical application of the monoclonal antibodies targeted anticancer drugs is the price .
3.Synthesis and biological evaluation of a series of 2-(((5-akly/aryl-1-pyrazol-3-yl)methyl)thio)-5-alkyl-6-(cyclohexylmethyl)-pyrimidin-4(3)-ones as potential HIV-1 inhibitors.
Yumeng WU ; Chengrun TANG ; Ruomei RUI ; Liumeng YANG ; Wei DING ; Jiangyuan WANG ; Yiming LI ; Christopher C LAI ; Yueping WANG ; Ronghua LUO ; Weilie XIAO ; Hongbing ZHANG ; Yongtang ZHENG ; Yanping HE
Acta Pharmaceutica Sinica B 2020;10(3):512-528
A series of 2-(((5-akly/aryl-1-pyrazol-3-yl)methyl)thio)-5-alkyl-6-(cyclohexylmethyl)-pyrimidin-4(3)-ones were synthesized and their anti-HIV-1 activities were evaluated. Most of these compounds were highly active against wild-type (WT) HIV-1 strain (IIIB) with EC values in the range of 0.0038-0.4759 μmol/L. Among those compounds, had an EC value of 3.8 nmol/L and SI (selectivity index) of up to 25,468 indicating excellent activity against WT HIV-1. anti-HIV-1 activity and resistance profile studies suggested that compounds and displayed potential anti-HIV-1 activity against laboratory adapted strains and primary isolated strains including different subtypes and tropism strains (ECs range from 4.3 to 63.6 nmol/L and 18.9-219.3 nmol/L, respectively). On the other hand, it was observed that those two compounds were less effective with EC values of 2.77 and 4.87 μmol/L for HIV-1A (K103N + Y181C). The activity against reverse transcriptase (RT) was also evaluated for those compounds. Both and obtained sub-micromolar IC values showing their potential in RT inhibition. The pharmacokinetics examination in rats indicated that compound has acceptable pharmacokinetic properties and bioavailability. Preliminary structure-activity relationships and molecular modeling studies were also discussed.