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Derivatives of Amaryllidaceae alkaloids and their biological activity: Derivatives of maritidine
Moravcová, Markéta ; Cahlíková, Lucie (advisor) ; Kuneš, Jiří (referee)
Charles University Faculty of Pharmacy in Hradec Králové Department of Pharmacognosy and Pharmaceutical Botany Candidate: Markéta Moravcová Supervisor: prof. Ing. Lucie Cahlíková, Ph.D. Title of diploma thesis: Derivatives of Amaryllidaceae alkaloids and their biological activity: derivatives of maritidine The object of this diploma thesis was the preparation a pilot series of semisynthetic derivatives and screenink of their biological activities. Ten aromatic esters of maritidine were prepared. The compounds were identified by LC-MS, HR-MS, NMR analysis, and optical rotation. All prepared analogues matridine were screened for in vitro inhibitory activity against hAChE and hBuChE. Most of the derivatives were inactive, only the 3-O-(4-ethylbenzoyl)maritidine derivative showed moderate activity against hBuChE with IC50 = 67.01 ± 3.12 μM. Two derivatives maritidine, 3-O-(3,5-dimethylbenzoyl)maritidine and 3-O-(3,5- dimethoxybenzoyl)maritidine, were tested for their antimycobacterial activity. The substances showed promising antimycobacterial activity against Mtb H37Ra strain (MICs = 7.81 and 15.625 µg/ml). These two derivatives maritidine were tested against different strains of microorganisms. 3-O-(3,5-dimethylbenzoyl)maritidine showed antimicrobial activity against Staphylococcus aureus (MIC =...
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