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Methods Mol Biol. 2020;2089:257-286. doi: 10.1007/978-1-0716-0163-1_18.

Cholinesterase as a Target for Drug Development in Alzheimer's Disease.

Author information

1
Pharmaceutical Chemistry Research Laboratory, Department of Pharmaceutical Engineering and Technology, Indian Institute of Technology (Banaras Hindu University), Varanasi, India.
2
Pharmaceutical Chemistry Research Laboratory, Department of Pharmaceutical Engineering and Technology, Indian Institute of Technology (Banaras Hindu University), Varanasi, India. skshrivastava.phe@itbhu.ac.in.

Abstract

Alzheimer's disease (AD) is an enormous healthcare challenge, and 50 million people are currently suffering from it. There are several pathophysiological mechanisms involved, but cholinesterase inhibitors remained the major target from the last 2-3 decades. Among four available therapeutics (donepezil, rivastigmine, galantamine, and memantine), three of them are cholinesterase inhibitors. Herein, we describe the role of acetylcholine sterase (AChE) and related hypothesis in AD along with the pharmacological and chemical aspects of the available cholinesterase inhibitors. This chapter discusses the development of several congeners and hybrids of available cholinesterase inhibitors along with their binding patterns in enzyme active sites.

KEYWORDS:

Acetylcholine; Acetylcholinesterase; Acyl binding pocket; Amyloid beta; Anionic subsite; Butyrylcholine; Butyrylcholinesterase; Catalytic active site; Choline acetyltransferase; Donepezil; Galantamine; N-Benzylpiperidine; Oxyanion hole; Peripheral anionic site; Rivastigmine; Tacrine

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