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
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.
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
Decisions concerning a project’s expedition, traditionally involved considerations regarding time and cost tradeoff. It was recently suggested that the quality of a project should also be taken into considerations. In this paper, we propose a meta-heuristic solution procedure for the discrete time, cost and quality tradeoff problem. This problem involves the scheduling of project activities in order to minimize the total cost of the project while maximizing the quality of the project and also meeting a given deadline. We apply a so called electromagnetic scatter search to solve this problem. In this process, we initially generate a population of feasible solutions. In so doing, we use frequency memory to well sample the feasible region. A number of these solutions are then selected and improved locally. The improved solutions are then combined to generate new set of solutions. The combination process utilizes attraction–repulsion mechanisms borrowed from the electromagnetism theory. The whole process is stopped when no significant improvement in the set of solutions are observed. The validity of the proposed solution procedure is demonstrated, and its applicability is tested on a randomly generated large and complex problem having 19,900 activities. 相似文献
3,4-Diformyl-2,5-dimethylpyrrole (1) reacts with ,ω-diamino-alkanes, NH2(CH2)nNH2t' to form either the potentially tautomeric 2:2 macrocyclic adduct (7a) (8), when N = 2, or the potentially tautomeric 1:1 bicyclic adduct (18) (19), when N = 4, 5, 6, and 12. 1H and 13C N.m.r. spectral data indicate that the 2-azafulvene structures predominate for both types of cycloadducts. Only polymeric material was obtained when N = 3. 相似文献
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