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• W3205323704 endingPage "1604" @default.
• W3205323704 startingPage "1604" @default.
• W3205323704 abstract "Monoamine oxidase B (MAO-B) metabolizes dopamine and plays an important role in oxidative stress by altering the redox state of neuronal and glial cells. MAO-B inhibitors are a promising therapeutical approach for Parkinson's disease (PD). Herein, 24 melatonin analogues (3a-x) were synthesized as novel MAO-B inhibitors with the potential to counteract oxidative stress in neuronal PC12 cells. Structure elucidation, characterization, and purity of the synthesized compounds were performed using 1H-NMR, 13C-NMR, HRMS, and HPLC. At 10 µM, 12 compounds showed >50% MAO-B inhibition. Among them, compounds 3n, 3r, and 3u-w showed >70% inhibition of MAO-B and IC50 values of 1.41, 0.91, 1.20, 0.66, and 2.41 µM, respectively. When compared with the modest selectivity index of rasagiline (II, a well-known MAO-B inhibitor, SI > 50), compounds 3n, 3r, 3u, and 3v demonstrated better selectivity indices (SI > 71, 109, 83, and 151, respectively). Furthermore, compounds 3n and 3r exhibited safe neurotoxicity profiles in PC12 cells and reversed 6-OHDA- and rotenone-induced neuronal oxidative stress. Both compounds significantly up-regulated the expression of the anti-oxidant enzyme, heme oxygenase (HO)-1. Treatment with Zn(II)-protoporphyrin IX (ZnPP), a selective HO-1 inhibitor, abolished the neuroprotective effects of the tested compounds, suggesting a critical role of HO-1 up-regulation. Both compounds increased the nuclear translocation of Nrf2, which is a key regulator of the antioxidative response. Taken together, these data show that compounds 3n and 3r could be further exploited for their multi-targeted role in oxidative stress-related PD therapy." @default.
• W3205323704 created "2021-10-25" @default.
• W3205323704 creator A5004061152 @default.
• W3205323704 creator A5029646455 @default.
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• W3205323704 creator A5034951384 @default.
• W3205323704 creator A5046385170 @default.
• W3205323704 creator A5051553362 @default.
• W3205323704 creator A5052093812 @default.
• W3205323704 creator A5077137801 @default.
• W3205323704 creator A5081639618 @default.
• W3205323704 date "2021-10-12" @default.
• W3205323704 modified "2023-10-13" @default.
• W3205323704 title "Melatonin Analogues Potently Inhibit MAO-B and Protect PC12 Cells against Oxidative Stress" @default.
• W3205323704 cites W1068320829 @default.
• W3205323704 cites W1166587220 @default.
• W3205323704 cites W1461736289 @default.
• W3205323704 cites W1504584187 @default.
• W3205323704 cites W1567084126 @default.
• W3205323704 cites W1588992136 @default.
• W3205323704 cites W1967539305 @default.
• W3205323704 cites W1971513938 @default.
• W3205323704 cites W1977403821 @default.
• W3205323704 cites W1979022173 @default.
• W3205323704 cites W1982666490 @default.
• W3205323704 cites W1985460799 @default.
• W3205323704 cites W1992326577 @default.
• W3205323704 cites W2000510440 @default.
• W3205323704 cites W2003048870 @default.
• W3205323704 cites W2009584071 @default.
• W3205323704 cites W2015859691 @default.
• W3205323704 cites W2022768159 @default.
• W3205323704 cites W2042386533 @default.
• W3205323704 cites W2045416175 @default.
• W3205323704 cites W2047547987 @default.
• W3205323704 cites W2049588777 @default.
• W3205323704 cites W2052522958 @default.
• W3205323704 cites W2053100374 @default.
• W3205323704 cites W2054051710 @default.
• W3205323704 cites W2054253103 @default.
• W3205323704 cites W2063087688 @default.
• W3205323704 cites W2066254885 @default.
• W3205323704 cites W2067657132 @default.
• W3205323704 cites W2069885465 @default.
• W3205323704 cites W2074028222 @default.
• W3205323704 cites W2074833985 @default.
• W3205323704 cites W2076897791 @default.
• W3205323704 cites W2081218759 @default.
• W3205323704 cites W2095511769 @default.
• W3205323704 cites W2098619885 @default.
• W3205323704 cites W2100004854 @default.
• W3205323704 cites W2100837265 @default.
• W3205323704 cites W2104285755 @default.
• W3205323704 cites W2111629536 @default.
• W3205323704 cites W2118857937 @default.
• W3205323704 cites W2125160631 @default.
• W3205323704 cites W2127303641 @default.
• W3205323704 cites W2133050346 @default.
• W3205323704 cites W2137508090 @default.
• W3205323704 cites W2142115579 @default.
• W3205323704 cites W2148214085 @default.
• W3205323704 cites W2155634762 @default.
• W3205323704 cites W2156930225 @default.
• W3205323704 cites W2158817614 @default.
• W3205323704 cites W2220635816 @default.
• W3205323704 cites W2479394673 @default.
• W3205323704 cites W2510865085 @default.
• W3205323704 cites W2522859355 @default.
• W3205323704 cites W2566927390 @default.
• W3205323704 cites W2576001856 @default.
• W3205323704 cites W2586368171 @default.
• W3205323704 cites W2589255768 @default.
• W3205323704 cites W2593436234 @default.
• W3205323704 cites W2674325859 @default.
• W3205323704 cites W2750818786 @default.
• W3205323704 cites W2760716489 @default.
• W3205323704 cites W2765290339 @default.
• W3205323704 cites W2766790825 @default.
• W3205323704 cites W2769184579 @default.
• W3205323704 cites W2774793916 @default.
• W3205323704 cites W2787324869 @default.
• W3205323704 cites W2790776869 @default.
• W3205323704 cites W2792448780 @default.
• W3205323704 cites W2793283287 @default.
• W3205323704 cites W2794460349 @default.
• W3205323704 cites W2889759397 @default.
• W3205323704 cites W2892098973 @default.
• W3205323704 cites W2897344568 @default.
• W3205323704 cites W2898985510 @default.
• W3205323704 cites W2909808393 @default.
• W3205323704 cites W2911646646 @default.
• W3205323704 cites W2936059353 @default.
• W3205323704 cites W2944764789 @default.
• W3205323704 cites W2947696479 @default.
• W3205323704 cites W2953248198 @default.
• W3205323704 cites W2953304185 @default.
• W3205323704 cites W2955561447 @default.
• W3205323704 cites W2972186560 @default.

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