Ahmed Hazem Abdelazeem

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Methamphetamine interacts with sigma receptors at physiologically relevant concentrations suggesting a potential site for pharmacologic intervention. In the present study, a previous sigma receptor ligand, CM156, was optimized for metabolic stability, and the lead analog was evaluated against the behavioral effects of methamphetamine. Radioligand binding(More)
Evaluation of management of the displaced intra-articular calcaneal fractures (DIACF) Sanders types II and III by using minimally invasive sinus tarsi approach and fixation by screws only technique. Open reduction using the limited lateral approach and internal fixation using screws only was studied in 33 patients with unilateral isolated simple DIACF with(More)
The purpose of this study was to describe the technique and clinical results following the utilization of biomechanical and biological means for adequate fracture healing in management of non-union of the neck of femur while preventing distortion of normal hip biomechanics. Twenty-two patients with non-united fractures of femoral neck in adults were treated(More)
Methamphetamine abuse continues as a major problem in the USA owing to its powerful psychological addictive properties. AZ66, 3-[4-(4-cyclohexylpiperazine-1-yl)pentyl]-6-fluorobenzo[d]thiazole-2(3H)-one, an optimized sigma receptor ligand, is a promising therapeutic agent against methamphetamine. To study the in vivo pharmacokinetics of this novel sigma(More)
A novel set of 4-substituted-1-phenyl-pyrazolo[3,4-d]pyrimidine and 5-substituted-1-phenyl-pyrazolo[3,4-d]pyrimidin-4-one derivatives were synthesized and evaluated as potential anti-inflammatory agents. The newly prepared compounds were assessed through the examination of their in vitro inhibition of four targets; cyclooxygenases subtypes (COX-1 and(More)
AIM Energy-restriction mimetic agents (ERMAs) are small-molecule agents that target various aspects of energy metabolism, which has emerged as a promising approach in cancer therapy. In the current study, we tested the ability of OSU-CG5, a novel ERMA, to target human colorectal cancer (CRC) in vitro. METHODS Two human CRC cell lines (HCT-116 and Caco-2)(More)
Glucokinase (GK) has received recent interest as a valid antidiabetic target. With this in mind, we applied a computational workflow based on combining pharmacophore modeling and QSAR analysis followed by in silico screening toward the discovery of novel GK activators. Virtual screening identified 10 promising bioactivators from the National Cancer(More)
Human neutrophil elastase inhibitors (HNE-Is) have been recently implicated in inflammatory diseases. Accordingly, we applied a drug discovery workflow to unveil novel inhibitory HNE leads via combining pharmacophore modeling, quantitative structure–activity relationship (QSAR) analysis, and in silico screening. We employed the pharmacophoric models and(More)
The identification of sigma receptor (σR) subtypes has been based on radioligand binding and, despite progress with σ1R cellular function, less is known about σR subtype functions in vivo. Recent findings that cocaine self administration experience will trigger σR agonist self administration was used in this study to assess the in vivo receptor subtype(More)
A series of diphenylthiazole-thiazolidinone hybrids was synthesized and evaluated in vitro and in vivo as anti-inflammatory/analgesic agents. The inhibition of cyclooxygenase (COX) enzymes was suggested as a molecular mechanism for the hybrids to exert their anti-inflammatory action. Of these compounds, 13b, 14, and 15b showed the most potent COX inhibitory(More)