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1.
Journal of Thermal Analysis and Calorimetry - In recent decades, the growth of heat transfer using nanomaterials in the conventional base fluid has caught the attention of researchers...  相似文献   
2.

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.

  相似文献   
3.
 Under intrinsic and extrinsic curvature assumptions on a Riemannian spin manifold and its boundary, we show that there is an isomorphism between the restriction to the boundary of parallel spinors and extrinsic Killing spinors of non-negative Killing constant. As a corollary, we prove that a complete Ricci-flat spin manifold with mean-convex boundary isometric to a round sphere, is necessarily a flat disc. Received: 2 February 2002; in final form: 1 August 2002 / Published online: 1 April 2003 Mathematics Subject Classification (1991): 53C27, 53C40, 53C80, 58G25 The authors would like to thank Lars Andersson for helpful discussions and for bringing to our knowledge the information regarding Remark 4. We are also grateful to the referee for pointing out that Corollary 5 and Corollary 6 are only valid when the boundary is at least 2-dimensional. Research of S. Montiel is partially supported by a Spanish MCyT grant No. BFM2001-2967  相似文献   
4.
The singlet oxygen (1Δg) photooxidations of angelic acid salt (1), tiglic acid salt (2), 2,3-dimethyl-2-butenoic acid salt (3), 3-ethoxycarbonyl-5,6-dihydro-2-methyl-4H-pyrane acid salt (4), cis-3-hexenoic acid salt (5), and trans-3-hexenoic acid salt (6) were conducted in deuterated water. The major and minor ene allylic hydroperoxide products were quantified and indicate that the allylic hydrogen geminal to the carboxylate group is preferentially abstracted in 1-4, whereas the allylic hydrogen α to the carboxylate is slightly favored for 5 and 6. We have attributed the observed regiochemistry in 1-4 to stabilizing hydrogen bonding interactions between the solvent and the perepoxide, which leads to the major ene product.  相似文献   
5.
A narrow bandwidth ring dye laser pumped by an argon ion laser has been used to investigate the hyperfine structure of the even and odd parity levels of tantalum by optogalvanic spectroscopy in the wavelength range 5640 to 6050 Å. Seventeen transitions have been observed and eight of these have not been reported in the literature so far. These transitions involve 27 levels with 15 odd and 12 even parity configurations. The magnetic dipole hyperfine interaction constants A and the electric quadrupole interaction constants B for these levels have been computed and compared with the data available in literature. The results for the levels at 34799.71 cm?1, 26960.46 cm?1 and 19657.78 cm?1 are reported for the first time.  相似文献   
6.
A new method for the rapid and sensitive determination of trace quantities of thiocyanate based on its Landolt effect on the bromate-hydrochloric acid reaction was developed. The induction period of the reaction is proportional to the SCN concentration. The decolorization of methyl orange by the reaction products was used to monitor the reaction spectrophotometrically at 525 nm. We were able to determine thiocyanate in the range 2 × 10–7–4 × 10–5 M by this method. The relative standard deviation for 10 determinations of 1.5 × 10–6 M thiocyanate ion is 0.19% and the detection limit of the method was 7.00 × 10–8 M. The method was applied to the determination of thiocyanate in human blood serum and of saliva samples with satisfactory results.  相似文献   
7.
Neutron induced radiography has been applied to the determination of boron concentrations in drinking water, collected from natural springs of Reshian and Muzaffarabad areas of Azad Kashmir, Pakistan, using CR-39 etched track detectors. The technique is based upon the simultaneous irradiation with thermal neutrons of a sample of unknown concentration and a standard of known boron concentration, fixed on a track detector. The subsequent counting of alpha and 7Li tracks in the detector resulting from the 10B(n,)7Li nuclear reaction is done after chemical etching. Boron concentration in the sample is determined by comparing 7Li and alpha-particle track density with that of a standard of known boron concentration. Boron concentrations in drinking water samples from Muzaffarabad and Reshian area of Azad Kashmir have been found to vary from (0.054±0.001) mg/l to (0.250±0.004) mg/l with an average of (0.16±0.002) mg/l. The observed concentration of boron in drinking water has been found to be less than the provisional Maximum Acceptable Concentration level (0.4 mg//l) of WHO. The drinking water from the reported area has been found to be within safe limits as far as boron related health hazards are concerned.This revised version was published online in November 2005 with corrections to the Cover Date.  相似文献   
8.
9.
The shift of the Q-band of sodium zinc(II)-2,9,16,23-phthalocyanine tetracarboxylate (ZnPc(COONa)4) to about 800 nm is attributed to the influence of the electron-donating property of the carboxylate groups substituted in the β–position. ZnPc(COONa)4 which was found to have a symmetry of D 2h characterized by a splitting of the Q transition. This splitting was interpreted by the formation of dianionic symmetric ZnPc(COONa)4 resulting from the dissociation of the pyrrole protons as well as the possibility of Na+ dissolution of ZnPc(COONa)4 in the aqueous solution of NaOH.  相似文献   
10.
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