In order to find more safe and effective new anti-epileptic drugs, a series of 5-alkoxy (phenoxy) tetrazolo[1,5-a]quinazoline derivatives was synthesized using 2,4-dichloroquinazoline as the starting material. Their anticonvulsant activities were evaluated by the maximal electroshock test (MES). Results demonstrated that most of the test compounds exhibited weak anticonvulsant activity. Taking into account that depression is [...]
Starting from phthalic anhydride, several new 3-amine-6-alkoxy(phenoxy)-[1,2,4]triazo-lo[3,4-a]phthalazine derivatives were synthesized as potent anti-inflammatory agent. Their anti-inflammatory activities were studied via the method of the xylene-induced ear edema in mice. The study showed that most of the synthsised compounds exhibited anti-inflammatory activity to a certain extent. Especially, the compounds 6h (3-amine-6-(2-chlorophenoxy)-[1,2, 4]triazolo[3,4-a]phthalazine) and 6s (3-amine6-(4-aminophenoxy)-[1,2,4]triazolo[3,4-a]phth-alazine) showed [...]
This thesis consists of two projects:one is chemical synthesis of new reagent Tbfinoc-Met-OH and using it as building block of ubiquitin in solid phase synthesis as well as the product purification helper; another is chemical synthesis of azabicyclo drug intermediates.In the first project, the new reagent Tbfmoc-Met-OH is synthesized in five steps, and then it [...]
Drug clinical trial (DCR) is to point to evaluate the efficacy and safety of drugs in the human body (patients or healthy volunteers), in order to confirm and reveal the experiment with the effect of medicines and adverse reaction, etc. Clinical trials on evaluation of new drug efficacy and safety play an irreplaceable role. The [...]
Paclitaxel (Taxol), which is extracted from Taxus, is the anticancer agent of taxane structure. PTX has the function of stabilizing microtubule, inhibiting mitotic division and inducing apoptosis, and is an efficient cells poisonous drug. In December 1992 the FDA approved Taxol for refractory ovarian cancer. Later, it is approved for breast cancer. Today it is [...]
Objective:Establish a model of rabbit vascular grafts on infrarenal abdominal aorta and administrate rapamycin through vascular adventitia; observe the pathological changes of the vessel grafts and the expression of a-actin, vWf, PCNA, p27kip1, and study its relationship with the proliferation of vascular smooth muscle cells; investigate the mechanism of rapamycin inhibiting restenosis and the feasibility [...]
Recently, the treatment of ocular ailments mostly needs local applications of drugs into the ocular cavity and tissues. However, highly sensitivity and effective protection mechanisms of eyes make the application of many pharmaceutical carriers limited. Thus, there is an urgent requirement for researchers to design effective drug carriers for local ocular delivery. In this study, [...]
Neuraminidase (NA) is an influenza virus surface glycoprotein with enzymatic activity of cleavage HA-sialic acid interaction to release new viral particles from host cells. This study is to establish cell-based and enzyme-based neuraminidase inhibitors (NAIs) evaluation models targeting to both wild-type and Tamiflu-resistent neuraminidase (NA) of the 2009 H1N1 Influenza A virus [A/California/04/2009(H1N1), short as [...]
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