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21.
In this work, a novel series of arylisoxazole‐phenylpiperazines were designed, synthesized, and evaluated toward acetylcholinesterase (AChE) and butyrylcholinesterase (BChE). Our results revealed that [5‐(2‐chlorophenyl)‐1,2‐oxazol‐3‐yl](4‐phenylpiperazin‐1‐yl)methanone ( 5c ) was the most potent AChE inhibitor with IC50 of 21.85 μm . It should be noted that most of synthesized compounds showed no BChE inhibitory activity and [5‐(2‐fluorophenyl)‐1,2‐oxazol‐3‐yl](4‐phenylpiperazin‐1‐yl)methanone ( 5a ) was the most active anti‐BChE derivative (IC50=51.66 μm ). Also, kinetic studies for the AChE and BChE inhibitory activity of compounds 5c and 5a confirmed that they have simultaneously bound to the catalytic site (CS) and peripheral anionic site (PAS) of both AChE and BChE. Furthermore, docking study of compound 5c showed desired interactions of that compound with amino acid residues located in the active and peripheral anionic sites. Compound 5c was also evaluated for its BACE1 inhibitory activity and demonstrated IC50=76.78 μm . Finally, neuroprotectivity of compound 5c on Aβ‐treated neurotoxicity in PC12 cells depicted low activity.  相似文献   
22.
Molecular and Cellular Biochemistry - Active neutrophils participate in innate and adaptive immune responses through various mechanisms, one of the most important of which is the formation and...  相似文献   
23.
Plant Cell, Tissue and Organ Culture (PCTOC) - Mentha spicata L., as a rich source of phenolic acids, is known for its therapeutic importance. Elicitors play a crucial role in biosynthetic pathways...  相似文献   
24.
Seven sesquiterpene lactone derivatives, diversolides A-G (1-7), together with two known compounds, diversin (8) and stigmasterol, were isolated from the roots of Ferula diversivittata. The structures of these compounds were elucidated by extensive spectroscopic methods including 1D-(1H and 13C) and 2D-NMR experiments (DQF-COSY, HSQC, HMBC, and NOESY) as well as high-resolution EIMS. Compounds 1, 4 and 6-8 were tested for their in vitro antifungal and antibacterial activities. Some of the tested compounds showed moderate antifungal and antibacterial activities with minimum inhibitory concentration (MIC) values from 40 to 80 μg/ml.  相似文献   
25.
Molecular Biology Reports - The changing epidemiology and decreasing susceptibility to first-line antibiotics, such as vancomycin and linezolid, leave clinicians with few therapeutic options for...  相似文献   
26.
Alzheimer's disease (AD) is a well‐known neurodegenerative disorder affecting millions of old people worldwide and the corresponding epidemiological data emphasize the importance of the disease. As AD is a multifactorial illness, various single target directed drugs that have reached clinical trials have failed. Therefore, various factors associated with outset of AD have been considered in targeted drug discovery. In this work, various benzochromenoquinolinones were synthesized and evaluated for their cholinesterase and BACE1 inhibitory activities as well as neuroprotective and metal‐chelating properties. Among the synthesized compounds, 14‐amino‐13‐(3‐nitrophenyl)‐2,3,4,13‐tetrahydro‐1H‐benzo[6,7]chromeno[2,3‐b]quinoline‐7,12‐dione ( 6m ) depicted the best inhibitory activity toward acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) with IC50s of 0.86 and 6.03 μm , respectively. Also, the compound could inhibit β‐secretase 1 (BACE1) with IC50=19.60 μm and showed metal chelating ability toward Cu2+, Fe2+, and Zn2+. In addition, docking study demonstrated desirable interactions of compound 6m with amino acid residues characterizing AChE, BChE, and BACE1.  相似文献   
27.
The n-butanolic fraction of a methanolic extract (80%) from aerial parts of Ajuga chamaecistus ssp. tomentella was analysed using different chromatographic methods. Column (CC) and high-performance liquid chromatography (HPLC) were used for isolation and purification. 13C, H NMR, H-H COSY, HSQC, HMBC, and ESI-MS were employed for identification of the compounds isolated from this fraction. The structures of the compounds were determined to be cis-melilotoside (1), trans-melilotoside (2), lavandulifolioside (3), 20-hydroxyecdysone (4), leonoside B (5), martynoside (6), ajugalactone (7), makisterone A (8), and 24-dehydroprecyasterone (9). This is the first report on the presence of cis- and trans-melilotoside in Ajuga species. Cytotoxic evaluation of the n-butanolic fraction, cis- and trans-melilotoside against cancer (T47D, HT-29, and Caco-2) and normal (NIH 3T3) cell lines by the mitochondrial tetrazolium test (MTT) showed no cytotoxic effects up to 400 microg/mL. The results of this study suggest that melilotoside, phenylethyl glycosides, and phytoecdysteroids are the main constituents of the n-butanolic fraction of Ajuga chamaecistus ssp. tomentella.  相似文献   
28.
For practical use of perovskite solar cells (PSCs) the instability issues of devices, attributed to degradation of perovskite molecules by moisture, ions migration, and thermal‐ and light‐instability, have to be solved. Herein, highly efficient and stable PSCs based on perovskite/Ag‐reduced graphene oxide (Ag‐rGO) and mesoporous Al2O3/graphene (mp‐AG) composites are reported. The mp‐AG composite is conductive with one‐order of magnitude higher mobility than mp‐TiO2 and used for electron transport layer (ETL). Compared to the mp‐TiO2 ETL based cells, the champion device based on perovskite/Ag‐rGO and SrTiO3/mp‐AG composites shows overall a best performance (i.e., VOC = 1.057 V, JSC = 25.75 mA cm?2, fill factor (FF) = 75.63%, and power conversion efficiency (PCE) = 20.58%). More importantly, the champion device without encapsulation exhibits not only remarkable thermal‐ and photostability but also long‐term stability, retaining 97–99% of the initial values of photovoltaic parameters and sustaining ≈93% of initial PCE over 300 d under ambient conditions.  相似文献   
29.
Biotechnology Letters - Serotype 2 of dengue virus (DENV-2) is the most prevalent cause of dengue fevers. In this study, the C-prM gene was used for specific detection of DENV-2 by RT-LAMP assay....  相似文献   
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