Synthesis of several derivatives of methylthiophosphonic acids, cholinesterase inhibitors

1968 ◽  
Vol 17 (3) ◽  
pp. 565-568
Author(s):  
A. A. Abduvakhabov ◽  
N. N. Godovikov ◽  
M. I. Kabachnik
Keyword(s):  
Cholinesterase Inhibitors ◽  
Derivatives Of

Acetamide Derivatives of Chromen-2-ones as Potent Cholinesterase Inhibitors

2017 ◽  
Vol 350 (8) ◽  
pp. 1700076 ◽  
Author(s):  
Suchita Prasad ◽  
Bipul Kumar ◽  
Shiv Kumar ◽  
Karam Chand ◽  
Shashank S. Kamble ◽  
...  
Keyword(s):  
Cholinesterase Inhibitors ◽  
Derivatives Of

Phosphorylated Derivatives of Alkaloids and Nitrogen-containing Heterocycles — Cholinesterase Inhibitors

1983 ◽  
Vol 52 (10) ◽  
pp. 918-930 ◽  
Author(s):  
Abid S Sadykov ◽  
D N Dalimov ◽  
Nikolai N Godovikov
Keyword(s):  
Cholinesterase Inhibitors ◽  
Derivatives Of

scholarly journals Benzobicyclo[3.2.1]octene Derivatives as a New Class of Cholinesterase Inhibitors

Molecules ◽  
2020 ◽  
Vol 25 (21) ◽  
pp. 4872
Author(s):  
Tena Čadež ◽  
Ana Grgičević ◽  
Ramiza Ahmetović ◽  
Danijela Barić ◽  
Nikolina Maček Hrvat ◽  
...  
Keyword(s):  
Ring Opening ◽  
Structural Adjustment ◽  
Cholinesterase Inhibitors ◽  
Furan Ring ◽  
Phenyl Substituent ◽  
Oxime Ether ◽  
New Class ◽  
Further Development ◽  
Derivatives Of ◽  
Acyl Derivatives

A library of amine, oxime, ether, epoxy and acyl derivatives of the benzobicyclo[3.2.1]octene were synthesized and evaluated as inhibitors of both human acetylcholinesterase (AChE) and butyrylcholinesterase (BChE). The majority of the tested compounds exhibited higher selectivity for BChE. Structural adjustment for AChE seems to have been achieved by acylation, and the furan ring opening of furo-benzobicyclo[3.2.1]octadiene results for compound 51 with the highest AChE affinity (IC50 = 8.3 µM). Interestingly, its analogue, an oxime ether with a benzobicyclo[3.2.1]-skeleton, compound 32 was one of the most potent BChE inhibitors in this study (IC50 = 31 µM), but not as potent as endo-43, an ether derivative of the benzobicyclo[3.2.1]octene with an additional phenyl substituent (IC50 = 17 µM). Therefore, we identified several cholinesterase inhibitors with a potential for further development as potential drugs for the treatment of neurodegenerative diseases.

Carbamate Derivatives of Indolines as Cholinesterase Inhibitors and Antioxidants for the Treatment of Alzheimer’s Disease

2012 ◽  
Vol 55 (23) ◽  
pp. 10700-10715 ◽  
Author(s):  
Inessa Yanovsky ◽  
Efrat Finkin-Groner ◽  
Andrey Zaikin ◽  
Lena Lerman ◽  
Hila Shalom ◽  
...  
Keyword(s):  
Alzheimer’S Disease ◽  
Alzheimer's Disease ◽  
Cholinesterase Inhibitors ◽  
Derivatives Of

scholarly journals Novel 16-substituted bifunctional derivatives of huperzine B: multifunctional cholinesterase inhibitors

2009 ◽  
Vol 30 (8) ◽  
pp. 1195-1203 ◽  
Author(s):  
Yu-fang Shi ◽  
Hai-yan Zhang ◽  
Wei Wang ◽  
Yan Fu ◽  
Yu Xia ◽  
...  
Keyword(s):  
Cholinesterase Inhibitors ◽  
Derivatives Of

scholarly journals Identification of 4-aminoquinoline core for the design of new cholinesterase inhibitors

PeerJ ◽  
2016 ◽  
Vol 4 ◽  
pp. e2140 ◽  
Author(s):  
Yao Chen ◽  
Yaoyao Bian ◽  
Yuan Sun ◽  
Chen Kang ◽  
Sheng Yu ◽  
...  
Keyword(s):  
Small Molecules ◽  
Cholinesterase Inhibitor ◽  
Cholinesterase Inhibitors ◽  
Simple Structure ◽  
Therapeutic Strategies ◽  
Inhibitory Effects ◽  
Inhibitory Potency ◽  
Ache Inhibitors ◽  
Starting Point ◽  
Derivatives Of

Inhibition of acetylcholinesterase (AChE) using small molecules is still one of the most successful therapeutic strategies in the treatment of Alzheimer’s disease (AD). Previously we reported compound T5369186 with a core of quinolone as a new cholinesterase inhibitor. In the present study, in order to identify new cores for the designing of AChE inhibitors, we screened different derivatives of this core with the aim to identify the best core as the starting point for further optimization. Based on the results, we confirmed that only 4-aminoquinoline (compound 04 and 07) had cholinesterase inhibitory effects. Considering the simple structure and high inhibitory potency against AChE, 4-aminoquinoline provides a good starting core for further designing novel multifunctional AChEIs.

Synthesis and in vitro evaluation of new derivatives of 2-substituted-6-fluorobenzo[d]thiazoles as cholinesterase inhibitors

2013 ◽  
Vol 21 (7) ◽  
pp. 1735-1748 ◽  
Author(s):  
Aleš Imramovský ◽  
Vladimír Pejchal ◽  
Šárka Štěpánková ◽  
Katarína Vorčáková ◽  
Josef Jampílek ◽  
...  
Keyword(s):  
Cholinesterase Inhibitors ◽  
In Vitro Evaluation ◽  
Derivatives Of

scholarly journals Sulfonamide Derivatives of 2-Amino-1-phenylethane as Suitable Cholinesterase Inhibitors

2014 ◽  
Vol 13 (5) ◽  
pp. 739 ◽  
Author(s):  
MA Abbasi ◽  
S Ahmad ◽  
A Rehman ◽  
S Rasool ◽  
KM Khan ◽  
...  
Keyword(s):  
Cholinesterase Inhibitors ◽  
Derivatives Of
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