Abstract:
:With the purpose of expanding the structural variety of chemical compounds available as pharmacological tools for the treatment of Alzheimer's disease, we synthesized and evaluated a novel series of indole-benzoxazinones (Family I) and benzoxazine-arylpiperazine derivatives (Family II) for potential human acetylcholinesterase (hAChE) inhibitory properties. The most active compounds 7a and 7d demonstrated effective inhibitory profiles with Ki values of 20.3 ± 0.9 μM and 20.2 ± 0.9 μM, respectively. Kinetic inhibition assays showed non-competitive inhibition of AChE by the tested compounds. According to our docking studies, the most active compounds from both series (Families I and II) showed a binding mode similar to donepezil and interact with the same residues.
journal_name
Arch Pharm (Weinheim)journal_title
Archiv der Pharmazieauthors
Méndez-Rojas C,Quiroz G,Faúndez M,Gallardo-Garrido C,Pessoa-Mahana CD,Chung H,Gallardo-Toledo E,Saitz-Barría C,Araya-Maturana R,Kogan MJ,Zúñiga-López MC,Iturriaga-Vásquez P,Valenzuela-Gutiérrez C,Pessoa-Mahana Hdoi
10.1002/ardp.201800024subject
Has Abstractpub_date
2018-05-01 00:00:00pages
e1800024issue
5eissn
0365-6233issn
1521-4184journal_volume
351pub_type
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