In this work, 2-alkyl-10-chloro-1,2,3,4-tetrahydrobenzo[][1,6]naphthyridines were obtained and their reactivity was studied. Novel derivatives of the tricyclic scaffold, including 1-phenylethynyl (), 1-indol-3-yl (), and azocino[4,5-]quinoline () derivatives, were synthesized and characterized herein for the first time. Among the newly synthesized derivatives, - proved to be MAO B inhibitors with potency in the low micromolar range. In particular, the 1-(2-(4-fluorophenyl)ethynyl) analog achieved an IC of 1.35 μM, a value close to that of the well-known MAO B inhibitor pargyline.
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http://dx.doi.org/10.3390/molecules28041662 | DOI Listing |
Carbohydr Polym
March 2025
School of Chemistry and Materials Science, South-Central Minzu University, Wuhan 430074, China; School of Pharmaceutical Sciences, South-Central Minzu University, Wuhan 430074, China. Electronic address:
Fucosylated chondroitin sulfate (FCS) from Holothuria mexicana (FCS) was selected for investigation because of its intriguing branch features. Selective β-eliminative depolymerization and the bottom-up assembly were performed to unravel that FCS consisted of a {D-GlcA-β1,3-D-GalNAc} backbone and branches of alternating Fuc (55 %) and D-GalNAc-α1,2-L-Fuc (45 %), the highest proportion of disaccharide branch reported to date. In branches, sulfation could occur at every free -OH site except O-3 of GalNAc, being the most complex and various structure features of natural FCS.
View Article and Find Full Text PDFBiomedicines
November 2024
Centro Universitario de Los Lagos, Universidad de Guadalajara, Lagos de Moreno 47460, Jalisco, Mexico.
Pharmacotherapy for depression includes drugs such as monoamine oxidase inhibitors (MAOIs), tricyclic antidepressants (TCAs), selective serotonin reuptake inhibitors (SSRIs), noradrenaline (NA) and serotonin (5-HT) reuptake inhibitors (NaSSAs), and atypical antidepressants; these drugs exert differentially beneficial effects on symptoms of depression after acute and chronic treatment in animal models. Said effects are established through neuroplastic mechanisms involving changes in neurogenesis and synaptogenesis as result of the activation of intracellular signaling pathways associated with neurochemical and behavioral changes. Antidepressants increase the synaptic availability of monoamines (monoaminergic hypothesis) such as 5-HT, NA, and gamma-aminobutyric acid (GABA) by inhibiting their reuptake or degradation and activating intracellular signaling pathways such as the responsive element binding protein (cAMP-CREB) cascade, which regulates the expression of genes related to neuroplasticity and neurogenesis, such as brain-derived neurotrophic factor (BDNF), in various brain structures implicated in depression.
View Article and Find Full Text PDFRSC Adv
January 2025
Department of Chemistry, COMSATS University Islamabad, Abbottabad Campus 22060 Pakistan +92334517999 +923005316570.
It is believed that inflammation influences several physiological processes, including the function of the central nervous system. Moreover, the impairment of lipid mechanisms/pathways is associated with neurodegenerative disorders and onset of Alzheimer's disease (AD). AD is a chronic neurodegenerative disease representing the major cause of dementia worldwide.
View Article and Find Full Text PDFCNS Spectr
January 2025
Department of Psychiatry, University of Toronto, Toronto, ON, Canada.
Adv Healthc Mater
January 2025
Department of Neurosurgery, the Second Affiliated Hospital, School of Medicine, Zhejiang University, Hangzhou, Zhejiang, 310009, China.
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