Synthesis of piperidine-4-one Derivative Containing Dipeptide: An Acetyl cholinesterase and β-secretase Inhibitor | Bentham Science

Parasuraman Pavadai; Suresh Ramalingam; Theivendren Panneerselvam; Selvaraj Kunjiappan; Pandurangan Perumal; Vasudevan Mani; Govindaraj Saravanan; Veerachamy Alagarsamy; Damodar Nayak Ammunje; Jithendra Chimakurthy

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Synthesis of piperidine-4-one Derivative Containing Dipeptide: An Acetyl cholinesterase and β-secretase Inhibitor | Bentham Science

机译：哌啶-4-一种含二肽的衍生物的合成：乙酰胆碱酯酶和β-分泌酶抑制剂| Bentham Science.

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With the goal of developing Alzheimer's disease therapeutics, we have designedand synthesized novel piperidone fused dipeptide (DPPS) derivatives possessing dual action such as acetylcholinesterase(AChE) and beta-amyloid peptide (Aβ) aggregation inhibition. Designed peptide wassynthesized by solid phase peptide synthesis using FMOC chemistry protocol and characterized by massspectroscopy.Methods: The amino acid sequence in peptide was analyzed by LC-MS-MS. In silico docking analysis wascarried out using GLIDE software. The docking score using GLIDE was found to be -7.88 against AChEand -9.74 against BACE1 enzyme. In vitro enzyme inhibition assay was carried out for AChE enzyme andBACE1 enzyme.Results: The IC50 values of AChE inhibition and BACE1 of DPPS were found to be 0.4796 μM/ml and0.0154 μM/ml, respectively. The correlation of in silico and in vitro results showed that DPPS possessed agreater ability to inhibit BACE1 enzyme.

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来源
《Anti-infective agents》 |2020年第2期|共9页
作者
Parasuraman Pavadai; Suresh Ramalingam; Theivendren Panneerselvam; Selvaraj Kunjiappan; Pandurangan Perumal; Vasudevan Mani; Govindaraj Saravanan; Veerachamy Alagarsamy; Damodar Nayak Ammunje; Jithendra Chimakurthy;
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作者单位

Department of Pharmaceutical Chemistry Faculty of Pharmacy M.S. Ramaiah University of Applied;

Department of Pharmacy Annamalai University Faculty of Engineering and Technology Annamalai Nagar;

Department of Research and Development Saraswathi Institute of Medical Sciences;

Sir CV Raman-KS Krishnan International Research Center Kalasalingam University;

Department of Pharmaceutical Chemistry Faculty of Pharmacy Asian Institute of Medicine Science;

Department of Pharmacology and Toxicology College of Pharmacy Qassim University;

Department of Pharmaceutical Chemistry MNR College of Pharmacy Fasalwadi;

Department of Pharmaceutical Chemistry MNR College of Pharmacy Fasalwadi;

Department of Pharmacology Faculty of Pharmacy M.S. Ramaiah University of Applied Sciences MSR;

Department of Pharmaceutical Sciences Vignan’s Foundation for Science Technology &

Research;

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原文格式 PDF
正文语种 eng
中图分类药学;
关键词
Alzheimers disease; peptides; DPPS; enzyme inhibition; AChE; BACE1;

机译：阿尔茨海默病;肽;DPP;酶抑制;疼痛;Bace1;

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Synthesis of piperidine-4-one Derivative Containing Dipeptide: An Acetyl cholinesterase and β-secretase Inhibitor | Bentham Science

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