ABSTRACT
In order to find highly active antidiabetic agents, the 3-amino group of skeletal structure of thiazolidine-2,4-diones (TZDs) was modified to generate the new molecules TM1 and TM2 in the present research. The new molecules TM3-TM6 containing rhodanine structural units were designed based upon the bioisostere and combination principles. The target molecules TM7, which is similar to the traditional TZDs structurally, were designed by connecting the phenolic hydroxyl of the above target molecules to carbazole through a linker. All of these target compounds were synthesized successfully by selecting suitable synthetic routes with optimized procedures. The assay results of peroxisome proliferator activated receptor response element (PPRE) agonist activity revealed that the PPAR agonist activity was decreased due to the change of TZD ring. The assay of α-glucosidase inhibitory activity and protein tyrosine phosphatase-1B (PTP-1B) inhibitory activity showed that most of the seven serials target molecules have weak activities in vitro. However, 3 of the compounds exhibited strong PTP-1B inhibitory activities. TM2-6 exhibited the highest inhibitory activities, which reached 96.71% with IC50 1.48 mg·L-1. In addition, the toxicity prediction disclosed that the highly active compounds were almost non-toxic. These results provide a hint for the development of new antidiabetic
ABSTRACT
Thirty-three compounds were designed and synthesized directly from three-component, one-pot condensation of 1-(4-methylphenyl)ethanone and aromatic amines with some aromatic aldehydes. The chemical structures of the Mannich bases were confirmed by 1H NMR, IR and MS. The screening results of bioactivity indicated that all of these title compounds possessed the inhibitory activity at the concentration of 1×10-4 mol·L-1. Among them, the compound TM33 displayed the strongest bioactivity with the inhibition percentage of 60.3% against P338 cancer cell line at the concentration of 1×10-8 mol·L-1, and the value of the half maximal inhibitory concentration (IC50) was as low as 0.45 nmol·L-1. This study suggests a new type of potential anti-leukemia molecules.
ABSTRACT
Objective To investigate the clinical application of laparoscopic adrenalectomy and summarize the experience in laparoscopie adrenalectomy.Methods From August 2002 to March 2007,21 cases of benign adrenal tumors were treated with retroperitoneal laparoscopy in this hospital.There were 9 cases of adrenocortical adenoma, 7 cases of primary aldosteronism,3 cases of adenocorticol macronodular hyperplasia,1 case of pheochromccytoma,and 1 case of adrenal gangliocytoma.Results Retroperitoneal laparoscopy was successfully applied in 21 cases.Operating time was between 65 and 130min with an average of 95 min.All patients did not receive blood transfusion and had no obvious complications.Conclusion Laparoscopic adrenalectomy had the advantages of minimal morbidity,mini- mal postoperative discomfort and a short hospital stay,whieh had a good prospect for application in the clinical prac- tice.