Enzīmu inhibitoru modificēšana bakteriālo šūnapvalku caurspiešanās spēju uzlabošanai
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Latvijas Universitāte
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Abstract
Maģistra darba ietvaros ir apkopota literatūra par sideroforu struktūru, transportu caur baktēriju šūnu membrānām un to izmantošanas iespējām. Īpaša uzmanība pievērsta sideroforu konjugātiem ar antibiotikām. Aplūkotas sideromicīnu un to sintētisko analogu izmantošanas iespējas. Realizēta hidroksamāta tipa siderofora sintēze pēc literatūras apraksta un viena leicīna t-RNS sintetāzes inhibitora resintēze. Ar mērķi uzlabot šī inhibitora bakteriālo šūnapvalku caurspiešanās spēju iegūts gan tā bioizostērs, gan tā siderofora konjugāts.
The literature of siderophore structure, their transport through cell membrane and their application was summarized in this thesis. A particular attention was paid to the siderophore conjugates with antibiotics. The use of sideromycins and synthetic siderophore analogues were reviewed. The synthesis of hydroxamate-based siderophore described in literature and the re-synthesis of the inhibitor of the leucine t-RNA synthetase were realized. With the aim to improve the bacterial penetration cell membrane of the inhibitor its bioisostere and its siderophore conjugate was obtained.
The literature of siderophore structure, their transport through cell membrane and their application was summarized in this thesis. A particular attention was paid to the siderophore conjugates with antibiotics. The use of sideromycins and synthetic siderophore analogues were reviewed. The synthesis of hydroxamate-based siderophore described in literature and the re-synthesis of the inhibitor of the leucine t-RNA synthetase were realized. With the aim to improve the bacterial penetration cell membrane of the inhibitor its bioisostere and its siderophore conjugate was obtained.