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Anxiolytic-like Action of Selected 4-(Alkylamino)-3-nitrocoumarin Derivatives in BALB/c Mice.

Published on Apr 17, 2020in Chemistry & Biodiversity1.449
· DOI :10.1002/CBDV.202000206
Pavle J. Randjelović12
Estimated H-index: 12
,
Niko S. Radulović26
Estimated H-index: 26
(University of Niš)
+ 4 AuthorsSonja Ilić4
Estimated H-index: 4
Abstract
In this work we explored the possible polypharmacological potential of the already established antimicrobials against gastrointestinal pathogens, 4-(alkylamino)-3-nitrocoumarins, as antianxiety agents, using a battery of in vivo experiments. Three chosen coumarin derivatives, differing in the substituent (sec-butylamino, hexadecylamino, or benzylamino) at position 4, at the doses of 25, 50 and 100 mg kg-1, were evaluated in light/dark, open-field, horizontal wire and diazepam-induced sleep models using male BALB/c mice. Depending on the applied dose, all three tested coumarins displayed a noteworthy anxiolytic-like effect. 4-(sec-Butylamino)-3-nitro-2H-chromen-2-one (1), and 4-(hexadecylamino)-3-nitro-2H-chromen-2-one (2) could be recognized as true anxiolytics in the lowest applied dose, based on three tests, without exerting any sedative effects. Thus, the 3-nitrocoumarin core deserves further chemical diversity exploration in the "antianxiety" direction.
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: Nine unsymmetrical azines containing a coumarin moiety were prepared by the reaction of the hydrazone of 4-hydroxy-3-acetylcoumarin with differently substituted aromatic aldehydes. The azines were fully spectrally characterized, including a complete assignment of 1 H- and 13 C-NMR resonances, and were assessed for their acute toxicities in the Artemia salina model. Their free radical scavenging activities were tested in the DPPH assay, and in vitro antimicrobial activities were determined agai...
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