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1.
Journal of Fluorescence - Malachite green (MG) is a dye that has been presented to use as photosensitizers for photodynamic therapy (PDT). Nonlinear absorption coefficient (β) and nonlinear...  相似文献   
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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.

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4.
Zahra  S.  Shafaq  B.  Kanwal  B. 《Physics of Atomic Nuclei》2020,83(5):770-772
Physics of Atomic Nuclei - Based on the behavior of elastic scattering of proton and anti-proton at $$\sqrt{s}=1.96$$ TeV for squared four-momentum transfer $$0.26<{-}t<1.2($$ GeV...  相似文献   
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We consider the plane-strain buckling of a cylindrical shellof arbitrary thickness which is made of a Varga material andis subjected to an external hydrostatic pressure on its outersurface. The WKB method is used to solve the eigenvalue problemthat results from the linear bifurcation analysis. We show thatthe circular cross-section buckles into a non-circular shapeat a value of µ1 which depends on A1/A2 and a mode number,where A1 and A2 are the undeformed inner and outer radii, andµ1 is the ratio of the deformed inner radius to A1. Inthe large mode number limit, we find that the dependence ofµ1 on A1/A2 has a boundary layer structure: it is constantover almost the entire region of 0 < A1/A2 < 1 and decreasessharply from this constant value to unity as A1/A2 tends tounity. Our asymptotic results for A1 – 1 = O(1) and A1– 1 = O(1/n) are shown to agree with the numerical resultsobtained by using the compound matrix method.  相似文献   
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以金属硫酸氢盐M(HSO4)n(Ca(HSO4)2,Zn(HSO4)2和过硫酸氢钾制剂oxone○R)为催化剂催化醛、1,3-二羰基化合物和尿素进行缩合反应,在90℃及无溶剂的条件下高收率、一锅法合成了3,4-二氢嘧啶-2(1H)-酮.  相似文献   
7.
Summary An integrated process for producing liquid fuels from synthesis gas via a two-stage Fischer-Tropsch (FT) reaction is disclosed. An iron catalyst was used in the first bed of a fixed-bed reactor followed by a ruthenium promoted cobalt catalyst in the second bed. The activity and selectivity of the dual-bed system were assessed and compared with those using catalysts in a single bed system, separately. The methane selectivity in the dual-bed reactor was about 11% less compared to that of the single-bed system. The C5+ selectivity for the dual-bed reactor was 19.7% higher than that of the single-bed system.  相似文献   
8.
Some new N‐carbonyl, phosphoramidates with formula C6H5C(O)N(H)P(O)R2 (R = NC3H6 ( 1 ), NC6H12 ( 2 ), NHCH2CH=CH2 ( 3 ), N(C3H7)2 ( 4 )) and CCl3C(O)N(H)P(O)R′2 (R′ = NC3H6 ( 5 ), NHCH2CH=CH2 ( 6 )) were synthesized and characterized by 1H, 13C, 31P NMR and IR spectroscopy and elemental analysis. The structures were determined for compounds 1 and 2 . Compound 1 exists as two crystallographically independent molecules in crystal lattice. Both compounds 1 and 2 produced dimeric aggregates via intermolecular ‐P=O…H‐N‐ hydrogen bonds, which in compound 2 is a centrosymmetric dimer. In compounds with four‐membered ring amine groups, 3J(P,C)>2J(P,C), in agreement with our previous studies about five‐membered ring amine groups. Also, 3J(P,C) values in compounds 1 and 5 are greater than in compounds with five‐, six‐ and seven‐membered ring amine groups.  相似文献   
9.
Nitrilimines were prepared from N-arylhydrazono chlorides and reacted with -alanine yielding the corresponding amidrazones, which were treated with 1,1-carbonyldiimidazole in THF affording the hitherto unknown 3-acetyl-1-aryl-1,4,5,6-tetrahydro-1,2,4-triazepin-7-ones.  相似文献   
10.

The complex anatomy of teeth limits the accessibility and efficacy of regenerative treatments. Therefore, the application of well-known inducers as injectable hydrogels for the regeneration of the dentin-pulp complex is considered a promising approach. In this regard, this study aimed to develop an injectable hydrogel containing mineral trioxide aggregate (MTA). The injectable chitosan/oxidized-nanocrystalline cellulose/MTA (CS/OCNC/MTA) hydrogels were prepared, and the physicochemical properties of these hydrogels were evaluated by TGA, FTIR, Rheological analysis, and SEM. Moreover, the effect of MTA on the swelling and degradability of scaffolds was assessed. The proliferative effects of synthesized hydrogels were also determined on human dental pulp stem cells (hDPSCs) by MTT assay. For induction of differentiation and biomineralization in these cells, the alkaline phosphatase activity and Alizarin Red S staining tests were performed in the presence of fabricated scaffolds. The proliferation of hDPSCs was significantly increased in the presence of these hydrogels. Moreover, the addition of MTA to hydrogel structure dramatically improved the differentiation of hDPSCs. These results suggested that this novel injectable hydrogel provides appropriate physiochemical properties and can be considered a promising scaffold for regenerative endodontic procedures.

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