Journal of Thermal Analysis and Calorimetry - Efficient air-conditioning inside the cars is a challenge in automobile industry. Thermoelectric is one of the new methods for air cooling. It has many... 相似文献
A new series of quinolotacrine hybrids including cyclopenta- and cyclohexa-quinolotacrine derivatives were designed, synthesized, and assessed as anti-cholinesterase (ChE) agents. The designed derivatives indicated higher inhibitory effect on the acetylcholinesterase (AChE) with IC50 values of 0.285–100 µM compared to butyrylcholinesterase (BChE) with IC50 values of?>?100 µM. Of these compounds, cyclohexa-quinolotacrine hybrids displayed a little better anti-AChE activity than cyclopenta-quinolotacrine hybrids. Compound 8-amino-7-(3-hydroxyphenyl)-5,7,9,10,11,12-hexahydro-6H-pyrano[2,3-b:5,6-c'] diquinolin-6-one (6m) including 3-hydroxyphenyl and cyclohexane ring moieties exhibited the best AChE inhibitory activity with IC50 value of 0.285 µM. The kinetic and molecular docking studies indicated that compound 6m occupied both the catalytic anionic site (CAS) and peripheral anionic site (PAS) of AChE as a mixed inhibitor. Using neuroprotective assay against H2O2-induced cell death in PC12 cells, the compound 6h illustrated significant protection among the assessed compounds. In silico ADME studies estimated good drug-likeness for the designed compounds. As a result, these quinolotacrine hybrids can be very encouraging AChE inhibitors to treat Alzheimer’s disease.
Graphic abstract
A novel series of quinolotacrine hybrids were designed, synthesized, and evaluated against AChE and BChE enzymes as potential agents for the treatment of AD. The hybrids showed good to significant inhibitory activity against AChE (0.285–100 μM) compared to butyrylcholinesterase (BChE) with IC50 values of?>?100 μM. Among them, compound 8-amino-7-(3-hydroxyphenyl)-5,7,9,10,11,12-hexahydro-6H-pyrano[2,3-b:5,6-c′] diquinolin-6-one (6 m) bearing 3-hydroxyphenyl moiety and cyclohexane ring exhibited the highest anti-AChE activity with IC50 value of 0.285 μM. The kinetic and molecular docking studies illustrated that compound 6 m is a mixed inhibitor and binds to both the catalytic anionic site (CAS) and peripheral anionic site (PAS) of AChE.
We present an application of an improved speckle photography technique for spatially extended phase objects. A contour mapping of a thin lens displaying its phase variation is presented. A theoretical analysis is investigated followed by the experimental presentation. Reasonable interference fringes are obtained and compared with the fringes obtained for hot air. The phase information of the object is extracted using the point-by-point technique. 相似文献
A new convenient route to metal containing polymers is described. This method involves emulsion co(ter) polymerization of a polar hydrocarbon soluble monomer, N-isobutoxymethylacrylamide (IBMA), with styrene or styrene/butadiene, followed by addition of metals. Metal incorporation is effected by latex or solution techniques. Preparative, atomic adsorption, spectroscopic, film observation, and dilute solution data are presented in support of metal complexation. Structures for the complexes are proposed. 相似文献
Dynamics of an array of line defects interacting with a background elastic medium is studied in the linear regime. It is shown that the inertial coupling between the defects and the ambient phonons leads to an anomalous response behavior for the deformation modes of a defect-lattice, in the form of anisotropic and anomalous mass and elastic constants, resonant dissipation through excitation of phonons, and instabilities. The case of a single fluctuating line defect is also studied, and it is shown that it could lead to formation of shock waves in the elastic medium for sufficiently high frequency deformation modes.Received: 18 February 2003, Published online: 23 July 2003PACS:
63.20.Mt Phonon-defect interactions -
61.72.Bb Theories and models of crystal defects -
66.30.Lw Diffusion of other defects 相似文献
The rate enhancements of dephosphorylation of p-nitrophenyldiphenyl phosphate by comicelles of cetyltrimethylammonium bromide with a functional cosurfactant are due wholly to increased concentration of the nucleophile in the micelle. 相似文献
The problem of gamma ray spectrum analysis has been is studied. The difficulties encountered by different methods are explained. An empirical method which uses an experimental peak for the analysis of spectrum is developed. This method utilizes the simple algorithm of linear least squares and is able to analyze the multiplets. It gives more accurate results than other ones. It is well adapted for automatic treatment of gamma ray spectra by small computers. 相似文献
To demonstrate the additional utility of ultrafast magnetic resonance imaging (MRI) of the fetus in the evaluation of sonographically detected or equivocal fetal congenital anomalies.
Material and Methods
Twenty five pregnant women with ultrasound detected fetal congenital anomalies underwent ultrafast fetal MRI.
Results
MRI findings altered the diagnosis of two cases of giant arachnoid cyst and sizable interhemispheric cyst associated with agenesis of the corpus callosum. MRI added additional findings of occult spinal diastematomyelia in two out of four cases of Chiari/meningocele malformation. MRI revealed impaired sulcation and unilateral cleft palate in suspected case of Walker-Warburg syndrome. In the remaining 18 cases MRI confirmed the diagnosis of Meckel–Gruber syndrome in three cases, hydronephrosis in six cases, cerebral ventriculomegaly in five cases, isolated omphalocele in three cases and findings suggestive of aneuploidy in the last case.
Conclusion
Ultrasound is the screening method of choice for evaluation of the fetus. Ultrafast MRI is a complementary adjunctive modality with excellent tissue contrast that can image the fetus in multiple planes and add information in sonographically detected or equivocal congenital anomalies that may be significant to establish definitive accurate diagnosis and hence adequate management and counseling. 相似文献