Synthesis of Novel Benzo[b][1,6]naphthyridine Derivatives and Investigation of Their Potential as Scaffolds of MAO Inhibitors

Autor:	Larisa N. Kulikova, Ghulam Reza Raesi, Daria D. Levickaya, Rosa Purgatorio, Gabriella La Spada, Marco Catto, Cosimo D. Altomare, Leonid G. Voskressensky
Jazyk:	angličtina
Rok vydání:	2023
Předmět:	benzonaphthyridine activated alkynes MAO inhibitors Alzheimer’s disease Organic chemistry QD241-441
Zdroj:	Molecules, Vol 28, Iss 4, p 1662 (2023)
Druh dokumentu:	article
ISSN:	1420-3049
DOI:	10.3390/molecules28041662
Popis:	In this work, 2-alkyl-10-chloro-1,2,3,4-tetrahydrobenzo[b][1,6]naphthyridines were obtained and their reactivity was studied. Novel derivatives of the tricyclic scaffold, including 1-phenylethynyl (5), 1-indol-3-yl (8), and azocino[4,5-b]quinoline (10) derivatives, were synthesized and characterized herein for the first time. Among the newly synthesized derivatives, 5c–h proved to be MAO B inhibitors with potency in the low micromolar range. In particular, the 1-(2-(4-fluorophenyl)ethynyl) analog 5g achieved an IC50 of 1.35 μM, a value close to that of the well-known MAO B inhibitor pargyline.
Databáze:	Directory of Open Access Journals
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