Bioorganic chemistry.
Publisher:
Academic Press.. Amsterdam : Elsevier
Frequency: Bimonthly,
Country: United States
Language: English
Start Year:1971 -
ISSN:
0045-2068 (Print)
1090-2120 (Electronic)
0045-2068 (Linking)
1090-2120 (Electronic)
0045-2068 (Linking)
Impact Factor
5.1
2022
| NLM ID: | 1303703 |
| (OCoLC): | 01713886 |
| (DNLM): | B19040000(s) |
| Coden: | BOCMBM |
| Classification: | W1 BI876K |
Amiridine-piperazine hybrids as cholinesterase inhibitors and potential multitarget agents for Alzheimer’s disease treatment. We synthesized eleven new amiridine-piperazine hybrids 5a-j and 7 as potential multifunctional agents for Alzheimer's disease (AD) treatment by reacting N-chloroacetylamiridine with piperazines. The compounds displayed mixed-type reversible inhibition of acetylcholinesterase (AChE) and butyrylcholinesterase (BChE). Conjugates were moderate inhibitors of equine and human BChE with negligible fluctuation in anti-BChE activity, whereas anti-AChE activity was substantially dependent on N4-substitution of the piperazine ring. Compounds with para-substituted aromatic moieties (5g, 5h, and bis-amirid...