Abstract In this work, a novel series of arylisoxazole‐phenylpiperazines were designed, synthesized, and evaluated toward acetylcholinesterase (AChE) 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 IC 50 21.85 μ m . It should be noted synthesized compounds showed no BChE inhibitory activity [5‐(2‐fluorophenyl)‐1,2‐oxazol‐3‐yl](4‐phenylpiperazin‐1‐yl)methanone 5a active...

Abstract A novel series of hybrid arylisoxazole‐chromenone carboxamides were designed, synthesized, and evaluated for their cholinesterase (ChE) inhibitory activity based on the modified Ellman's method. Among synthesized compounds, 5‐(3‐nitrophenyl)‐ N ‐{4‐[(2‐oxo‐2 H ‐1‐benzopyran‐7‐yl)oxy]phenyl}‐1,2‐oxazole‐3‐carboxamide depicted most acetylcholinesterase (AChE) (IC 50 =1.23 μ m ) 5‐(3‐chlorophenyl)‐ was found to be potent butyrylcholinesterase (BChE) inhibitor =9.71 )....

Considering the global incidence of diabetes, developing new compounds to lower blood sugar levels has become increasingly crucial. As a result, there been growing focus on synthesis α-glucosidase inhibitors in recent years. This study investigated design, synthesis, and effects novel 5-aryl pyrazole-glucose hybrids as inhibitors. Thirteen derivatives from this class were synthesized, demonstrating superior vitro inhibitory (IC50 values ranging 0.5 438.6 µM, compared acarbose at 750.0 µM)....

Abstract Herein, various N′ -substituted benzylidene benzohydrazide-1,2,3-triazoles were designed, synthesized, and screened for their inhibitory activity toward α-glucosidase. The structure of derivatives was confirmed using 1 H- 13 C-NMR, FTIR, Mass spectrometry, elemental analysis. All exhibited good inhibition with IC 50 values in the range 0.01 to 648.90 µM, compared acarbose as positive control (IC = 752.10 µM). Among them, compounds 7a 7h showed significant potency 0.02 respectively....

Alzheimer's disease (AD) remains a significant public health challenge due to its progressive cognitive impairment and the absence of proven treatments. In this study, several novel 1,2,3-triazole-methoxyphenyl-1,3,4-oxadiazole derivatives were synthesized evaluated for their ability inhibit key enzymes associated with AD: acetylcholinesterase (AChE) butyrylcholinesterase (BChE). Structure-activity relationship (SAR) analysis revealed that featuring electron-withdrawing groups, particularly...

Alzheimer's disease (AD) is a progressive neurodegenerative disorder characterized by cholinergic dysfunction, neuroinflammation, oxidative stress, and memory impairment. The Salvia genus has been used since ancient times for its anti-inflammatory neuroprotective properties. In this study, we aimed to investigate the effects of aristata hydroalcoholic extract (SAHE) dichloromethane (SADE) on various aspects AD. Column chromatography was utilized in phytochemical analysis isolate purify...

Abstract In search of safer tacrine analogs, various thieno[2,3‐ b ]pyridine amine derivatives were synthesized and evaluated for their inhibitory activity against cholinesterases (ChEs). Among the compounds, compounds 5e 5d showed highest towards acetylcholinesterase butyrylcholinesterase, with IC 50 values 1.55 0.23 µM, respectively. The most active ChE inhibitors ( ) also candidates further complementary assays, such as kinetic molecular docking studies well on amyloid‐beta (βA)...

The plants from Salvia genus contain widely distributed species which have been used in folk medicine as well pharmaceutical and food industries.The chemical composition of 12 native Iranian (14 plants) was identified using gas chromatography-mass spectrometry (GC-MS). Also, the inhibitory activity all essential oils (EOs) evaluated toward α-glucosidase two types cholinesterase (ChE) spectrophotometric methods. vitro inhibition assay performed by determination p-nitrophenol (pNP) obtained...

Alzheimer's disease (AD) is a well-known neurodegenerative disorder affecting millions of old people worldwide and the corresponding epidemiological data emphasize importance disease. As AD multifactorial illness, various single target directed drugs that have reached clinical trials failed. Therefore, factors associated with outset been considered in targeted drug discovery. In this work, benzochromenoquinolinones were synthesized evaluated for their cholinesterase BACE1 inhibitory...

In order to develop effective anti-cholinesterase compounds, a novel series of pyrano[3',4':5,6]pyrano[2,3-b]quinolinones were designed, synthesized, and evaluated in vitro against acetylcholinesterase (AChE) butyrylcholinesterase (BChE). All derivatives showed very good AChE inhibitory (AChEI) activity (IC50 = 0.37-5.62 μM) compared with rivastigmine 11.07 μM). Among them, 11-amino-12-(2,3-dichlorophenyl)-3-methyl-7,8,9,10-tetrahydropyrano[3',4':5,6]pyrano[2,3-b]quinolin-1(12H)-one (6f)...

Abstract The complex pathophysiology of Alzheimer's disease (AD) has prompted researchers to develop multitarget‐directed molecules find an effective therapy against the disease. In this context, a novel series N ‐(1‐benzylpiperidin‐4‐yl)‐5‐arylisoxazole‐3‐carboxamide derivatives were designed, synthesized, and evaluated acetylcholinesterase (AChE) butyrylcholinesterase (BuChE). vitro biological evaluation demonstrated that compound 4e was best AChE (IC 50 = 16.07 μM) BuChE inhibitor 15.16...

Abstract Novel series of fused 1,4‐dihydropyridine derivatives were designed and synthesized. Oxidized to the corresponding pyridines these dihydropyridines. Both dihydropyridines evaluated as acetyl butyrylcholinesterase inhibitors. outperformed against enzyme, but none had a suitable inhibitory effect acetylcholinesterase. Among 1,4‐dihydropyridines, compounds derived from vanillin ( 4 j – p ) inhibited (BChE) with IC 50 values 2.87–15.61 μM, 4‐hydroxybenzaldehyde did not show...

Abstract: Carbohydrates are an important group of biomolecules that have received special attention due to their significant role in the design and synthesis new bioactive compounds. In this study, a class 5-arylisoxazole-glucose hybrids was designed synthesized for evaluation inhibitory effects on α-glucosidase, α-amylase, tyrosinase. The target compounds depicted selective α-glucosidase activity over which is factor reducing probable gastrointestinal problems treatment type 2 diabetes....

Aim: A new series of 1,2,3-triazole-hydrazone derivatives were developed to evaluate their anti-Alzheimer's activity. Materials & methods: All compounds screened toward cholinesterases via the modified Ellman's method. The toxicity assay on SH-SY5Y cells was performed using MTT assay, and expression levels GSK-3α, GSK-3β, DYRK1 CDK5 assessed in presence 6m 6p. Results: 6p; acting as mixed-type inhibitors, exhibited promising acetylcholinesterase butyrylcholinesterase inhibitory activity,...

Alzheimer's disease (AD) is a progressive mental disorder that brings huge economic burden to the healthcare systems. During this illness, acetylcholine levels in cholinergic systems gradually diminish, which results severe memory loss and cognitive impairments. Moreover, Butyrylcholinesterase (BuChE) enzyme participates neurotransmission regulation by playing prominent role latter phase of AD. In study, based on donepezil, an effective acetylcholinesterase (AChE) inhibitor, series...

In this work, n-hexane, chloroform, and ethyl acetate fractions of the methanol extract Myristica fragrans Houtt. seeds were evaluated against acetylcholinesterase (AChE) butyrylcholinesterase (BChE) via Ellman's method. It was found that all depicted no anti-AChE activity, however, they active toward BChE with IC50 values 361.8, 215.0, 145.8 µg/mL, respectively comparing donepezil as reference drug (IC50 = 1.97 µg/mL). The fraction which also showed high neuroprotectivity metal chelating...

Background: Thiazole derivatives are known as important sulfur containing heterocycles which present in a wide range of biologically active natural products. Keywords: Heterocycles, inhibitory activity, 15-LOX, synthesis, thiazolones.

Background: Alzheimer’s disease (AD), the main form of dementia, is a multifactorial neurodegenerative disease, and several hypotheses have been proposed for its pathogenesis. Among them, cholinergic hypofunction reason plays significant role in cognitive impairment. According to this theory, ChE inhibitors improve performance system increase memory function. Thus, study investigated novel series 2-amino-pyrano[3,2-c]quinoline-3-carbonitrile derivatives bearing benzyloxy phenyl moiety as...