Design, biological evaluation, molecular docking study and in silico ADME prediction of novel imidazo[2,1-b]thiazole derivatives as a novel class of α-glucosidase inhibitors

Inhibiting the degradation of carbohydrates into glucose is considered to be an effective treatment for type 2 diabetes mellitus. Herein, a series of novel thiosemicarbazide and 1,2,4-triazole-3-thione derivatives of imidazo[2,1-b]thiazole were synthesized and evaluated for their α-glucosidase inhibitory activity. Compound5c(IC50: 4.54 ± 0.19 µM) was found approximately 47 times more active thanAcarbose(IC50: 214.71 ± 8.34 µM). In addition to thein vitroanalysis, molecular docking studies were employed to explore the possible binding interactions of the title compounds. Structure-activity relationships, as well as virtual ADME studies, were carried out and a relationship between biological, electronic, and physicochemical qualifications of the target compounds was determined. Consequently, our studies indicated that these imidazo[2,1-b]thiazole derivatives possess the potential of being a novel class of α-glucosidase inhibitors

Comparison of Tramadol, Diclofenac and Fentanyl in Combination with Propofol for Dilatation and Curettage: A Retrpospective Study

Aim: The aim of our study was to compare the effects of preoperative use of tramadol, diclofenac and fentanyl in combination with propofol on hemodynamics, propofol requirements, recovery and post-operative pain in patients undergoing dilatation and curettages. Methods: After approval of the Ethics Committee, 90 patients aged 18-70 years, who had undergone a dilatation and curettage between April 2009 and March 2011, were included in the study. The subjects were divided into three groups: group D consited of patients who received diclofenac 100 mg intramuscularly 30 minutes before induction, group T received tramadol 100 mg intravenously 15 minutes before induction and the patients in group F were administered fentanyl 1 µgr/kg intravenously for induction. Induction was provided with propofol 2 mg/kg and the total doses of propofol required were recorded. Preoperative and postoperative hemodynamic parameters and SpO2 readings were recorded. The patients were evaluated using a visual analog scale (0-10), the Ramsay Sedation Scale (0-6), and the Aldrete Recovery Scale (0-10) at the 1st, 5th, 10th, 120th minutes postoperatively. Results: The mean postoperative systolic blood pressure and the mean arterial blood pressure were significantly lower in group F. In the first minute, Aldrete recovery scores were significantly lower in G, group D and group T. Propofol consumption was significantly lower in group F. Conclusion: Fentanyl decreased the propofol requirements and increased the recovery score accordingly. Hypotension should be considered in high-risk patients. There was no statistically significant difference between the groups regarding effectiveness of analgesia. It is concluded that each can be used alternatively prior to dilatation and curettage. (The Me­di­cal Bul­le­tin of Ha­se­ki 2014; 52: 10-13