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Structural modification of haemanthamine
Babcová, Jitka ; Cahlíková, Lucie (advisor) ; Kuneš, Jiří (referee)
Charles University Faculty of Pharmacy in Hradec Králové Department of Pharmacognosy and Pharmaceutical Botany Candidate: Jitka Babcová Supervisor: prof. Ing. Lucie Cahlíková, Ph.D. Title of diploma thesis: Structural modification of haemanthamine The object of this diploma thesis was to prepare several derivates of alkaloid haemanthamine. Twelve aromatic esters of haemanthamine and two ethers were prepared. Compounds were identified by MS, NMR analysis and optical rotation and screened for their biological activities. Ten prepared derivates were screened for in vitro inhibitory activity againts hAChE and hBuChE. All derivates were considered inactive (IC50 ˃ 10 µM). Twelve derivates of haemanthamine were tested for thein antimycobacterial aktivity, using rifampicin as a standard. The most interesting antimycobacterial potencial against Mtb H37Ra strain has shown 11-O-(4-pentylbenzoyl)haemanthamine (MIC = 3,91 µg/ml), against M. aurum: 11-O-(4-tercbutyllbenzoyl)haemanthamine, 11-O-(1-naftoyl)haemanthamine a 11-O-(4-butylbenzoyl)haemanthamine (MICs = 7,81 µg/ml), against M. avium: 11-O-(4-pentylbenzoyl)haemanthamine, 11-O-(4-hexylbenzoyl)haemanthamine (MICs = 31,25 µg/ml), against M. kansasii: 11-O-(4-pentylbenzoyl)haemanthamine (MIC = 3,91 µg/ml), 11-O-(4-hexylbenzoyl)haemanthamine (MIC = 7,81...
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