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Hit, Lead & Candidate Discovery
A variety of novel 2-(methyl/phenyl)-3-(4-(5-substituted-1,3,4-oxadiazol-2-yl)phenyl) quinazolin-4(3H)-ones have been synthesized by treating 3-(4-(5-mercapto-1,3,4-oxadiazol-2-yl)phenyl)-2-(methyl/phenyl)-quinazolin-4(3H)-one with a variety of secondary amines. Graph theoretical analysis was used in identification of drug target that is, NMDAR (N-methyl-d -aspartate receptors). The observed reports of in silico modeling and ligand based toxicity, metabolism prediction studies were encouraging us to synthesize of title compounds and evaluate their antiepileptic effects. The title compounds were tested for its antiepileptic potency by MES and scPTZ model. Rotorod test is used to assess its neurotoxicity. In the preliminary test it was found that in MES test, analogs 6d , 6e , 6f, and 6l were potent; whereas in scPTZ test analogs 6d , 6e , 6f, and 6k displayed potent antiepileptic activity. Additionally these five derivatives were tested in rats orally at a dose of 30 mg/kg and found that compounds 2-methyl-3-(4-(5-morpholino-1,3,4-oxadiazol-2-yl)phenyl)quinazolin-4(3H)-one 6e and 2-methyl-3-(4-(5-(piperidin-1-yl)-1,3,4-oxadiazol-2-yl)phenyl)quinazolin-4(3H)-one 6f exhibited superior activity than reference Phenytoin. In MES test, these derivatives 6e and 6f showed activity at 30 mg/kg i.p. dose after 0.5 hr and 4.0 hr. In scPTZ test these derivatives 6e and 6f showed activity at 100 and 300 mg/kg i.p. dose after 0.5 hr and 4.0 hr, respectively.  相似文献   
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Purpose: To study the role of Optical coherence tomography (OCT) Angiography (OCTA) in detecting retinal vascular and macular abnormalities as compared to Fundus Fluorescein Angiography (FFA) in subjects with Asteroid hyalosis (AH).

Methods: In a prospective study, patients with AH underwent OCTA and FFA. AH graded as Grade 1 in 8 (optic disc, second order vessels visible), Grade 2 in 4 (optic disc, first-order vessels visible), Grade 3 in 11 (hazy view of optic disc) and Grade 4 (no view of fundus) in 2 eyes.

Results: A total of 20 patients (25 eyes) with AH were included. In comparison to FFA, OCTA was able to similarly detect Diabetic Retinopathy changes such as Neovascularization, microaneurysms, capillary dropout, and foveal avascular zone extent in vascular occlusion in all grades of AH.

Conclusion: OCTA, a noninvasive imaging tool, could detect various retinal vascular and macular abnormalities in patients with all grades of AH in comparison to FFA.  相似文献   

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This study describes a new custom measurement system designed to investigate the biomechanics of sitting-pivot wheelchair transfers and assesses the reliability of selected biomechanical variables. Variables assessed include horizontal and vertical reaction forces underneath both hands and three-dimensional trunk, shoulder, and elbow range of motion. We examined the reliability of these measures between 5 consecutive transfer trials for 5 subjects with spinal cord injury and 12 nondisabled subjects while they performed a self-selected sitting pivot transfer from a wheelchair to a level bench. A majority of the biomechanical variables demonstrated moderate to excellent reliability (r > 0.6). The transfer measurement system recorded reliable and valid biomechanical data for future studies of sitting-pivot wheelchair transfers.We recommend a minimum of five transfer trials to obtain a reliable measure of transfer technique for future studies.  相似文献   
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Auricular reconstruction is an interdisciplinary approach where multiple specialties play a vital role in the treatment provided to the patient. This article provides a comprehensive interpretation of the process carried out for the fabrication of a custom‐made prosthetic conformer for the management of postoperative contraction of a skin graft after ear reconstruction surgery—Brent stage III. The prosthesis is used as a precautionary measure and is simple, effective, and economical.  相似文献   
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