Design, Synthesis and Evaluation of 8-Thiosubstituted 1,3,7-Trimethylxanthine Hydrazones with In Vitro Neuroprotective and MAO-B Inhibitory Activities.

Design, Synthesis and Evaluation of 8-Thiosubstituted 1,3,7-Trimethylxanthine Hydrazones with In Vitro Neuroprotective and MAO-B Inhibitory Activities. Med Chem. 2019 May 31;: Authors: Mitkov J, Kasabova-Angelova A, Kondeva-Burdina M, Tzankova V, Tzankova D, Georgieva M, Zlatkova A Abstract The syntheses and biological activities of 8-thiosubstituted-1,3,7-trimethylxanthine derivatives bearing an aromatic hydrazid-hydrazone fragment in the side chain at C8 are described. The chemical structures of the synthesized compounds 6a-m were confirmed based on their MS, FTIR, 1H NMR and 13C NMR analysis. The in vitro investigations of neuroprotective effects manifested on cellular (human neuroblastoma cell line SH-SY5Y) and sub-cellular (isolated rat brain synaptosomes) levels show that compounds 6g and 6i demonstrate statistically significant activity. The performed monoamine oxidase B (MAO-B) inhibition study in vitro show that compounds 6g and 6i possess a significant MAO-B inhibition activity close to L-deprenyl. These results suggest that such compounds may be utilized for the development of new candidate MAO-B inhibitors for treatment of Parkinson's disease. PMID: 31146671 [PubMed - as supplied by publisher]
Source: Medicinal Chemistry - Category: Chemistry Authors: Tags: Med Chem Source Type: research