A series of xanthene-based thiazoles was synthesized and characterized by different scpectroscopic methods, i.e. Proton nuclear magnetic resonance( 1 H NMR), carbon nuclear magnetic resonance ( 13 C NMR), infrared spectroscopy, carbon hydrogen nitrogen analysis, and X-ray crystallography. The inhibition potencies of 18 newly synthesized thiazole derivatives were investigated on the activities of acetylcholinesterase (AChE), butyrylcholinesterase (BChE), α-amylase (α-Amy), and α-glycosidase (α-Gly) enzymes in accordance with their antidiabetic and anticholinesterase ability. The synthesized compounds have the highest inhibition potential against the enzymes at low nanomolar concentrations. Among the 18 newly synthesized molecules, 3b and 3p were superior to the known commercial inhibitors of the enzymes and have a much more effective inhibitory potential, with IC 50 : 2.37 and 1.07 nM for AChE, 0.98 and 0.59 nM for BChE, 56.47 and 61.34 nM for α-Gly, and 152.48 and 124.84 nM for α-Amy, respectively. Finally, the optimized 18 compounds were subjected to molecular docking to describe the interaction between thiazole derivatives and AChE, BChE, α-Amy, and α-Gly enzymes in which important interactions were monitored with amino acid residues of each target enzyme.
Background: Ondansetron is a 5HT3 receptor blocker and has multifaceted action like sodium channel blocker and µ - opioid agonist. Objective: To compare the efficiency of ondansetron pre-treatment in alleviating pain caused by propofol during induction of general anaesthesia with placebo. Material & Method: In this randomized controlled trail 120 patients of ASA grade I & II undergoing elective surgery were included and divided into two equal groups A & B by using lottery method. Each group comprised of 60 patients. In group A two ml 0.9 % normal saline and in group B, 2 ml ondansetron (4mg) given intravenously. In both groups propofol was given in a dose of 2.5 mg / Kg intravenously. Results: The mean age of patients in group A was 29.95 ± 4.79 year and in group B was 30.30 ± 4.87 year. Majority of patients 67(55.83 %) were between 18 to 30 year of age. Out of 120 patients. 63 (52.50 %) were ASA I & 52 (47.50 %) were ASA II. Efficacy of group A (placebo) was seen in 11 (18.33 %) while in group B (ondansetron) was seen in 56 (93.33 %). Conclusion: Ondansetron pre-treatment in alleviating pain cause by propofol is very effective. Keywords: Pain, ondansetron, propofol, general anaesthesia.
Monoamine oxidase and cholinesterase enzymes are important targets for the treatment of several neurological diseases especially depression, Parkinson disease and Alzheimer's.
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