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Series of diaryl-based pyrazole and triazole derivatives were designed and synthesized in a facile synthetic approach in order to produce selective COX-2 inhibitor. These series of derivatives were synthesized by different reactions like Vilsmeier–Haack reaction and click reaction. In vitro COX-1 and COX-2 inhibition studies showed that five compounds were potent and selective inhibitors of the COX-2 isozyme with IC50 values in 0.551–0.002 μM range. In the diarylpyrazole derivatives, compound 4b showed the best inhibitory activity against COX-2 with IC50 = 0.017 μM as one of the N-aromatic rings was substituted with sulfonamide and the other aromatic ring was unsubstituted. However, when the N-aromatic ring was substituted with sulfonamide and the other aromatic ring was substituted with sulfone (compound 4d), best COX-2 selectivity was achieved (IC50 = 0.098 μM, SI = 54.847). In the diaryltriazole derivatives, compound 15a showed the best inhibitory activity in comparison to all synthesized compounds including the reference celecoxib with IC50 = 0.002 μM and SI = 162.5 as it could better fit the extra hydrophobic pocket which is present in the COX-2 enzyme. Moreover, the docking study supports the obtained SAR data and binding similarities and differences on both isozymes.

Background: The primary aim of this study was to examine the clinical characteristics and outcomes of older patients who underwent hip fracture repair surgery. The secondary aims were to assess the predictors of the choice of spinal or general anaesthesia and to explore the risk factors for all-cause mortality. Methods: This three-tertiary centres study was conducted at a tertiary care centre in Jordan. Clinical data include previous fracture history; medication details; comorbidities; surgical approach; and postoperative pain management. Results: Overall, 1084 patients who underwent hip fracture repair were included in this study. The mean age of patients was 78 years, and 55.2% were women. Twenty-four were treated with bisphosphonates before the fracture, whereas 30 were in steroid therapy. Overall, 61.8% of patients underwent spinal anaesthesia, whereas 38.2% underwent general anaesthesia. Spinal anaesthesia group had a lower prevalence of cardiovascular accidents (16.3% vs. 22.3%, p = 0.014) and Alzheimer’s (3.4% vs. 1.4%, p = 0.049) than the general anaesthesia group. In the spinal anaesthesia group, postoperative opioid administration (p = 0.025) and postoperative blood transfusion (p = 0.011) occurred more frequently than general anaesthesia group. In hospital, 30-day and all-cause mortality were comparable between both groups. Diabetes mellitus (HR = 2.6; 95%CI = 1.5–4.4; p = 0.001); cemented hip hemiarthroplasty (HR = 2.4; 95%CI = 1.1–5.1; p = 0.025); deep venous thrombosis/pulmonary embolism (HR = 5.0; 95%CI = 1.2–12.9; p = 0.001); and readmission within 1 month from surgery (HR = 3.6; 95%CI = 2.0–6.3; p < 0.001) were all significant predictors of mortality. Conclusions: This study provides insights into the outcomes and factors associated with different anaesthesia types in hip fracture repair surgery. The anaesthesia type does not affect all-cause mortality in patients undergoing hip fracture repair.