Design, synthesis and evaluation of semi- and thiosemicarbazides containing a methylxanthine moiety with in vitro neuroprotective and MAO-B inhibitory activities. Issue 1 (8th July 2022)

• Record Type: Journal Article
• Authors: Mitkov, Javor; Kondeva-Burdina, Magdalena; Peikova, Lily; Georgieva, Maya; Zlatkov, Alexander
• Is Part Of: Biotechnology, biotechnological equipment. Volume 36:Issue 1(2022)
• Page Start: 486
• Page End: 499
• Publication Date: 2022-07-08
• Subjects: xanthines -- monoamine oxidase B inhibition -- neurotoxicity -- neuroprotection; Biotechnology -- Periodicals; Biotechnology -- Periodicals; Biotechnology -- instrumentation -- Periodicals; Periodicals; 660.605
• DOI: 10.1080/13102818.2022.2098819
• Languages: English
• ISSNs: 1310-2818

Abstract

Abstract: This study is focused on determination of the most appropriate synthetic approach for obtaining series of theophylline-7-acetyl semi- and thiosemicarbazide hybrids by using the molecular hybridization strategy with and without a catalyst. The target derivatives were further investigated for their in vitro neurotoxic and neuroprotective effects on cellular and subcellular level, along with their possible MAO-B inhibitory activities. The results identified 2-(1, 3-dimethyl-2, 6-dioxo-2, 3, 6, 7-tetrahydro-1H-purin-7-yl)- N -[(methylcarbamo-thioyl)amino] acetamide (5 ) as the most promising structure for further in vivo evaluations with the lowest neurotoxicity and the highest neuroprotection and MAO B inhibitory activity of 28%. Graphical Abstract: UF0001 The results identified 2-(1, 3-dimethyl-2, 6-dioxo-2, 3, 6, 7-tetrahydro-1H-purin-7-yl)- N -[(methylcarbamothio-yl)amino]acetamide (5 ) as the most prospective structure for further in vivo evaluations with the lowest neurotoxicity and the highest neuroprotection and MAO B inhibitory activity of 28%.