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A simple, efficient, cost-effective, recyclable and green approach has been developed for the synthesis of new dihydropyrimidinone analogs via the Biginelli reaction. The methodology involves a multicomponent reaction catalyzed by "HPA-Montmorillonite-KSF" as a reusable and heterogeneous catalyst. This method gives an efficient and much improved modification of the original Biginelli reaction, in terms of yield and short reaction times under solvent free conditions. All the derivatives were subjected to cytotoxicity screening against a panel of four different human cancer cell lines viz. colon (Colo-205), prostate (PC-3), leukemia (THP-1) and lung (A549) to check their effect on percentage growth. MTT [3-(4,5-dimethylthiazol-yl)-diphenyl tetrazoliumbromide] cytotoxicity assay was employed to check IC50 values. Of the synthesized analogs, 16a showed the best activity with IC50 of 7.1 ± 0.8, 13.1 ± 1.4, 13.8 ± 0.9 and 14.7 ± 1.1 µM against lung (A549), leukemia (THP-1), prostate (PC-3) and colon (Colo-205) cancer lines, respectively. The 16a analog was further checked for its effect on cancer cell properties through clonogenic (colony formation) and scratch motility (wound healing) assays and thereby was found that it reduced both the colony formation and migratory properties of the lung cancer cell line (A549). Further, molecular docking studies were performed with 16a to show its binding mode.
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Background Awareness during general anesthesia is undesired and unanticipated patient wakefulness during surgery or recall of intraoperative events. Incidence of awareness in patients undergoing cardiac surgery is significantly higher than the overall incidence of 1% during general surgery. Awareness during cardiac surgery can be prevented by a number of methods. One such method is the supplemental, intraoperative use of sedative agents. Propofol, a bisubstituted phenol, is an intravenous general anesthetic that has been shown to reduce the incidence of awareness. Dexmedetomidine-an alpha2-adrenergic agonist with anxiolytic, opioid, and general anesthetic-sparing properties-is being considered for maintaining intraoperative depth of anesthesia. The purpose of this study was to evaluate the effect of dexmedetomidine on depth of anesthesia and to compare it with the effect of propofol in cardiac surgery. Methods This was a prospective, randomized, double-blind study conducted in a tertiary-care hospital. Sixty patients with American Society of Anesthesiologists (ASA) physical status I-III planned for elective open heart surgery were randomized into two groups of 30 patients each. Each patient of the dexmedetomidine group received an initial loading dose of dexmedetomidine at 1 mcg kg-1 over 10 minutes followed by infusion at the rate of 0.2-0.6 mcg kg-1 hr-1. Patients of the propofol group received propofol infusion at the rate of 0.25-1 mg kg-1 hr-1. An identical technique-of standard general anesthesia and routine physiological monitoring-was used in both groups. Bispectral scores were recorded at predetermined intervals during surgery and the target bispectral index (BIS) was kept at 50±10. The patients were assessed for awareness and recall 24 hours after tracheal extubation using the Brice Questionnaire. Results Intraoperative BIS scores remained within the target range in both groups; however, the BIS scores showed variable trends between the groups and were significantly lower in the dexmedetomidine group (p < 0.001). None of the patients in either group had recall of intraoperative events. Conclusion Administration of dexmedetomidine was as effective in reducing awareness and recall in cardiac surgery compared to propofol. Thus, dexmedetomidine can be used as an alternative sedative agent to prevent awareness and recall in cardiac surgery.
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BACKGROUND: Injuries to the craniovertebral junction (CVJ) are not uncommon, and are among the few skeletal injuries that carry a high mortality rate. Successful management of these injuries depends on familiarity with the normal anatomic relationships of this region, as well as prudent decision making regarding surgical versus conservative management alternatives. METHODS: The purpose of this study was to analyze the indications for conservative treatment of CVJ trauma and to analyze the outcomes. RESULTS: Eighty-eight patients admitted with CVJ injuries were managed conservatively. More than half were nearly neurologically intact on admission; 91% improved whereas 80% (excluding deaths/lost to follow) ultimately achieved bony union without surgical intervention. CONCLUSION: This study documents that conservative management of CVJ injuries in a select population can yield good clinical results.
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BACKGROUND: Post-craniectomy hydrocephalus in patients with intracranial hypertension is becoming a major concern for neurosurgeons because of the increasing number of hospital admissions for head trauma, stroke and other lesions which may lead to severe brain oedema requiring decompressive craniectomy. METHODS: We collected records of all the paediatric patients who developed hydrocephalus following decompressive craniotomy from October 2011 to October 2013 and analysed their clinical profiles. RESULTS: We had 3 patients in this group, ranging in age from 6 to 18 years; 1 patient died and the other 2 patients continue to remain in follow-up. CONCLUSION: Post-traumatic hydrocephalus is one of the rare complications of decompressive craniotomy; CSF diversion remains the only option for improvement in neurological status.
