scholarly journals A multifunctional therapeutic approach: Synthesis, biological evaluation, crystal structure and molecular docking of diversified 1H-pyrazolo[3,4-b]pyridine derivatives against Alzheimer's disease

2019 ◽  
Vol 175 ◽  
pp. 2-19 ◽  
Author(s):  
Tarana Umar ◽  
Shruti Shalini ◽  
Md Kausar Raza ◽  
Siddharth Gusain ◽  
Jitendra Kumar ◽  
...  
Keyword(s):  
Crystal Structure ◽  
Alzheimer’S Disease ◽  
Alzheimer's Disease ◽  
Molecular Docking ◽  
Therapeutic Approach ◽  
Biological Evaluation ◽  
Pyridine Derivatives

scholarly journals Synthesis, molecular docking, and biological evaluation of novel 2-pyrazoline derivatives as multifunctional agents for the treatment of Alzheimer's disease

MedChemComm ◽  
2019 ◽  
Vol 10 (6) ◽  
pp. 1018-1026 ◽  
Author(s):  
Oya Unsal-Tan ◽  
Tuba Tüylü Küçükkılınç ◽  
Beyza Ayazgök ◽  
Ayla Balkan ◽  
Keriman Ozadali-Sari
Keyword(s):  
Alzheimer’S Disease ◽  
Alzheimer's Disease ◽  
Molecular Docking ◽  
Biological Evaluation ◽  
Multifunctional Agents

A novel series of 2-pyrazoline derivatives were designed, synthesized, and evaluated for cholinesterase (ChE) inhibitory, Aβ anti-aggregating and neuroprotective activities.

scholarly journals A new guanylhydrazone derivative as a potential acetylcholinesterase inhibitor for Alzheimer's disease: synthesis, molecular docking, biological evaluation and kinetic studies by nuclear magnetic resonance

RSC Advances ◽  
2017 ◽  
Vol 7 (54) ◽  
pp. 33944-33952 ◽  
Author(s):  
Denise Cristian Ferreira Neto ◽  
Marcelle de Souza Ferreira ◽  
Elaine da Conceição Petronilho ◽  
Josélia Alencar Lima ◽  
Sirlene Oliveira Francisco de Azeredo ◽  
...  
Keyword(s):  
Alzheimer’S Disease ◽  
Alzheimer's Disease ◽  
Nuclear Magnetic Resonance ◽  
Molecular Docking ◽  
Magnetic Resonance ◽  
In Silico ◽  
Acetylcholinesterase Inhibitor ◽  
Kinetic Studies ◽  
Biological Evaluation ◽  
Nuclear Magnetic

Molecular docking, in silico studies and NMR show that the new guanylhydrazone is a promising compound for the treatment of Alzheimer's disease.

Synthesis, Biological Evaluation, and Molecular Docking of 8-imino-2-oxo-2H,8H-pyrano[2,3-f]chromene Analogs: New Dual AChE Inhibitors as Potential Drugs for the Treatment of Alzheimer's Disease

2016 ◽  
Vol 88 (1) ◽  
pp. 43-53 ◽  
Author(s):  
Jeelan Basha Shaik ◽  
Bhagath Kumar Palaka ◽  
Mohan Penumala ◽  
Siddhartha Eadlapalli ◽  
Manidhar Darla Mark ◽  
...  
Keyword(s):  
Alzheimer’S Disease ◽  
Alzheimer's Disease ◽  
Molecular Docking ◽  
Biological Evaluation ◽  
Ache Inhibitors

Memapsin 2, a drug target for Alzheimer's disease

2003 ◽  
Vol 70 ◽  
pp. 213-220 ◽  
Author(s):  
Gerald Koelsch ◽  
Robert T. Turner ◽  
Lin Hong ◽  
Arun K. Ghosh ◽  
Jordan Tang
Keyword(s):  
Crystal Structure ◽  
Alzheimer’S Disease ◽  
Alzheimer's Disease ◽  
Transition State ◽  
Amyloid Precursor Protein ◽  
Therapeutic Target ◽  
Drug Target ◽  
Aspartic Protease ◽  
Precursor Protein ◽  
Memapsin 2

Mempasin 2, a ϐ-secretase, is the membrane-anchored aspartic protease that initiates the cleavage of amyloid precursor protein leading to the production of ϐ-amyloid and the onset of Alzheimer's disease. Thus memapsin 2 is a major therapeutic target for the development of inhibitor drugs for the disease. Many biochemical tools, such as the specificity and crystal structure, have been established and have led to the design of potent and relatively small transition-state inhibitors. Although developing a clinically viable mempasin 2 inhibitor remains challenging, progress to date renders hope that memapsin 2 inhibitors may ultimately be useful for therapeutic reduction of ϐ-amyloid.

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