Synthesis, molecular docking, acetylcholinesterase and butyrylcholinesterase inhibitory potential of thiazole analogs as new inhibitors for Alzheimer disease

Rahim, Fazal; Javed, Muhammad Tariq; Ullah, Hayat; Wadood, Abdul; Taha, Muhammad; Ashraf, Muhammad; Quratulain, -; Khan, Muhammad Ajmal; Khan, Fahad; Mirza, Salma; Khan, Khalid Mohammed

doi:10.1016/j.bioorg.2015.08.002

Cited by 116 publications

(39 citation statements)

References 46 publications

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“…In the continuation of our work on enzyme inhibition [27][28][29][30][31][32] we synthesized biscoumarin analogs 1-18 and evaluated for a-glucosidase inhibitory potential. All of the eighteen (18) The structure activity relationship has been established.…”

Section: Biological Activitymentioning

confidence: 99%

“…Afterward, 25 lL of PNPG in phosphate buffer saline (5 mM) were added and pre-read of the plate was taken by using a microplate reader (Spectrostar Nano BMG Labtech, Germany). The reaction mixture was then incubated at 37°C for 30 min and change in absorbance at 405 nm was monitored up to 30 for a-glucosidase of Saccharomyces cerevisiae has not been solved up-to yet. Only a few homology models have been reported [33][34][35][36].…”

Section: Baker's Yeast A-glucosidase Inhibition Assaymentioning

confidence: 99%

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Synthesis, in vitro evaluation and molecular docking studies of biscoumarin thiourea as a new inhibitor of α-glucosidases

Zawawi

Taha

Ahmat

et al. 2015

Bioorganic Chemistry

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Section: Biological Activitymentioning

confidence: 99%

Section: Baker's Yeast A-glucosidase Inhibition Assaymentioning

confidence: 99%

Synthesis, in vitro evaluation and molecular docking studies of biscoumarin thiourea as a new inhibitor of α-glucosidases

Zawawi

Taha

Ahmat

et al. 2015

Bioorganic Chemistry

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“…The thiazole ring is another bioactive structure known for its broad spectrum of pharmacological activity and favored for its synthetic accessibility and flexibility. The biological diversity of this ring is based on cholinergic action, which has been supported by several publications investigating the effect of novel thiazole derivatives as cholinesterase inhibitors . Recently, a thiazole‐based selective acetyl cholinesterase inhibitor (AChEI) molecule, acotiamide hydrochloride, has been discovered to treat functional dyspepsia by enhancing the actions of cholinergic neurons located in the stomach .…”

Section: Introductionmentioning

confidence: 99%

Novel thiazole‐piperazine derivatives as potential cholinesterase inhibitors

Demirayak

Şahin

Ertaş

et al. 2019

Journal of Heterocyclic Chem

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Dementia is a cognitive disorder mostly associated with Alzheimer's disease (AD) in addition to being seen in many other diseases of the central nervous system (CNS). The limited number of drugs is not sufficient to provide adequate improvement to increase the quality of life of patients suffering from this symptom; therefore, all treatment options should be evaluated in detail. In this study, new molecules, [2‐(4‐(2/3/4‐substituted phenyl)piperazin‐1‐yl)‐4‐phenylthiazol‐5‐yl][3/4‐substituted phenyl]methanone derivatives (1‐44), were obtained and analyzed in terms of their anticholinesterase activities. Kinetic mode and molecular interactions were also evaluated. An enzyme inhibition study was undertaken on acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) using the Ellman method. Maestro program was used in molecular modeling studies. Forty‐four compounds were evaluated on AChE and BChE enzymes at 10−3 and 10−4 concentrations. The inhibition concentrations were calculated as 0.268μM to 2.104μM for six compounds (4, 5, 16, 27, 37, and 38) on AChE. Compound 5 including the 4‐methoxy substituent (IC50: 0.268μM) and compound 38 containing the 4‐methoxy and 3‐methyl substituents (IC50: 0.286μM) showed the highest AChE inhibitory activity. They were further examined in terms of hydrogen bonding with Arg296 and Ar‐Ar interaction with Trp286. The activity of compound 5 was also assessed in mixed‐type kinetic mode.

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“…Thiazole containing molecules are used as an antimicrobial drug, abafungin as antifungal drug, ritonavir as antiretroviral drug, thiazofurin and bleomycine as antineoplastic [10], antihistaminic, niridazole as schistosomicidal, and nitazoxanide as antiprotozoal [11]. Our group has already reported thiazole analogs as acetylcholinesterase and butyrylcholinesterase inhibitor [12], with hopes to further explore their potential as alpha-amylase inhibitor. In this regard here in the present study we are going to report thiazole analogs as potent alpha-amylase inhibiter.…”

Section: Introductionmentioning

confidence: 99%

Thiazole Based Carbohydrazide Derivatives as α-Amylase Inhibitor and Their Molecular Docking Study

Taha

Irshad

Imran

et al. 2019

Heteroatom Chemistry

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In this study we are going to present thiazole based carbohydrazide in search of potent antidiabetic agent as α-amylase inhibitors. Thiazole based carbohydrazide derivatives 1-25 have been synthesized, characterized by 1HNMR, 13CNMR, and EI-MS, and evaluated for α-amylase inhibition. Except compound 11 all analogs showed α-amylase inhibitory activity with IC50 values from 1.709 ± 0.12 to 3.049 ± 0.25 μM against the standard acarbose (IC50 = 1.637 ± 0.153 μM). Compounds 1, 10, 14, and 20 exhibited outstanding inhibitory potential with IC50 value 1.763 ± 0.03, 1.747 ± 0.20, 1.709 ± 0.12, and 1.948 ± 0.23 μM, respectively, compared with the standard acarbose. Structure activity relationships have been established for the active compounds. To get an idea about the binding interaction of the compounds, molecular docking studies were done.

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Synthesis, molecular docking, acetylcholinesterase and butyrylcholinesterase inhibitory potential of thiazole analogs as new inhibitors for Alzheimer disease

Cited by 116 publications

References 46 publications

Synthesis, in vitro evaluation and molecular docking studies of biscoumarin thiourea as a new inhibitor of α-glucosidases

Synthesis, in vitro evaluation and molecular docking studies of biscoumarin thiourea as a new inhibitor of α-glucosidases

Novel thiazole‐piperazine derivatives as potential cholinesterase inhibitors

Thiazole Based Carbohydrazide Derivatives as α-Amylase Inhibitor and Their Molecular Docking Study

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