PMID- 30706815
OWN - NLM
STAT- MEDLINE
DCOM- 20190424
LR  - 20190424
IS  - 1873-4294 (Electronic)
IS  - 1568-0266 (Linking)
VI  - 19
IP  - 4
DP  - 2019
TI  - Target Enzyme in Alzheimer's Disease: Acetylcholinesterase Inhibitors.
PG  - 264-275
LID - 10.2174/1568026619666190128125912 [doi]
AB  - Alzheimer's Disease (AD), affecting a large population worldwide is characterized 
      by the loss of memory and learning ability in the old population. The enzyme 
      Acetylcholinesterase Enzyme (AChE) is the key enzyme in the hydrolysis of the 
      neurotransmitter acetylcholine and is also the target of most of the clinically 
      used drugs for the treatment of AD but these drugs provide only symptomatic 
      treatment and have the limitation of loss of therapeutic efficacy with time. The 
      development of different strategies targeting the AChE enzyme along with other 
      targets like Butyl Cholinesterase (BChE), amyloid-beta (Abeta), beta-secretase-1 (BACE), 
      metals antioxidant properties and free radical scavenging capacity has been 
      focused in recent years. Literature search was conducted for the molecules and 
      their rational design which have shown inhibition for AChE and the other 
      abovementioned targets. Several hybrid molecules incorporating the main 
      sub-structures derived from diverse chemotypes like acridine, quinoline, 
      carbamates, and other heterocyclic analogs have shown desired pharmacological 
      activity with a good profile in a single molecule. It is followed by optimization 
      of the activity through structural modifications guided by structure-activity 
      relationship studies. It has led to the discovery of novel molecules 17b, 20, and 
      23 with desired AChE inhibition along with desirable activity against other 
      abovementioned targets for further pre-clinical studies.
CI  - Copyright(c) Bentham Science Publishers; For any queries, please email at 
      epub@benthamscience.net.
FAU - Saxena, Mridula
AU  - Saxena M
AD  - Amity School of Applied Sciences, Amity University, Lucknow-226010, India.
FAU - Dubey, Ragini
AU  - Dubey R
AD  - Amity School of Applied Sciences, Amity University, Lucknow-226010, India.
LA  - eng
PT  - Journal Article
PT  - Review
PL  - United Arab Emirates
TA  - Curr Top Med Chem
JT  - Current topics in medicinal chemistry
JID - 101119673
RN  - 0 (Cholinesterase Inhibitors)
RN  - EC 3.1.1.7 (Acetylcholinesterase)
SB  - IM
MH  - Acetylcholinesterase/*metabolism
MH  - Alzheimer Disease/*drug therapy/*enzymology
MH  - Cholinesterase Inhibitors/chemistry/*pharmacology
MH  - Drug Discovery
MH  - Humans
MH  - *Molecular Targeted Therapy
MH  - Structure-Activity Relationship
OTO - NOTNLM
OT  - Acetylcholinesterase
OT  - Alzheimer's disease
OT  - Amyloid-beta- peptides
OT  - Molecular hybridization
OT  - Multi-target-directed ligands
OT  - Target enzyme.
EDAT- 2019/02/02 06:00
MHDA- 2019/04/25 06:00
CRDT- 2019/02/02 06:00
PHST- 2018/10/31 00:00 [received]
PHST- 2019/01/18 00:00 [revised]
PHST- 2019/01/18 00:00 [accepted]
PHST- 2019/02/02 06:00 [pubmed]
PHST- 2019/04/25 06:00 [medline]
PHST- 2019/02/02 06:00 [entrez]
AID - CTMC-EPUB-96174 [pii]
AID - 10.2174/1568026619666190128125912 [doi]
PST - ppublish
SO  - Curr Top Med Chem. 2019;19(4):264-275. doi: 10.2174/1568026619666190128125912.