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.
Arylation of the readily available 3‐alkythio‐5‐aryl‐1,2,4‐triazoles gave 5‐alkylthio‐1,3‐diaryl‐1,2,4‐triazoles in moderate yield. The structures of the latter were confirmed by NOE and 13C‐NMR. 相似文献
Multiply-connected monolayered cyclofusene (MMC) is a fused hexacyclic system with an exterior region and at least two interior empty regions called holes, as in figure 1. Each hexacyle has either: (a) two edges belonging to an exterior boundary and at least one hole, or (b)
two edges belonging to boundaries of at least two holes. Let G be the graph of a given MMC. We show that G is equitable if and only if the set of vertices belonging to three hexacycles is equitable. 相似文献
In this paper, the multi-item, single-level, capacitated, dynamic lot sizing problem with set-up carry-over and backlogging, abbreviated to CLSP+, is considered. The problem is formulated as a mixed integer programming problem. A heuristic method consisting of four elements: (1) a demand shifting rule, (2) lot size determination rules, (3) checking feasibility conditions and (4) set-up carry-over determination, provides us with an initial feasible solution. The resulting feasible solution is improved by adopting the corresponding set-up and set-up carry-over schedule and re-optimizing it by solving a minimum-cost network flow problem. Then the improved solution is used as a starting solution for a tabu search procedure, with the value of moves assessed using the same minimum-cost network problem. Computational results on randomly generated problems show that the algorithm, which is coded in C++, is able to provide optimal solutions or solutions extremely close to optimal. The computational efficiency makes it possible to solve reasonably large problem instances routinely on a personal computer. 相似文献
Preparation of 2-amino-N-(1-H-benzimidazol-2-yl)benzamide and a variety of new 3-(2-benzimidazolyl)-2-alkyl-4-(3H)-quinazolinones using isatoic anhydride, 2-aminobenzimidazole and orthoesters under microwave irradiation are described. 相似文献