Sinteza etilsečninskih derivatov benzotiazol-2-amina kot zaviralcev bakterijskih topoizomeraz

Roškar, Sara (author), Zega, Anamarija (mentor)

V okviru diplomske naloge smo sintetizirali etilsečninske derivate benzotiazol-2-amina, ki so imeli različne substituente na mestu 6. Namen različnih funkcionalnih skupin je bil izboljšanje topnosti spojin in tvorba interakcij z aminokislinskima ostankoma Arg76 in Arg136, saj so ključne za doseganje dobrega zaviralnega učinka. Strukturo in čistoto končne spojine smo preverili s kromatografskimi in spektroskopskimi metodami ter jim ovrednotili zaviralno aktivnost na izoliranem encimu DNA girazi iz bakterijske vrste Escherichia coli (E. coli).

• Language: Slovenian
• Keywords: bakterijska rezistenca, DNA giraza, etilsečninski derivati, zaviralci
• Work type: Bachelor thesis/paper
• Organization: FFA - Faculty of Pharmacy
• Year: 2022
• PID: 20.500.12556/RUL-141547
• Publication date in RUL: 01.10.2022

Secondary language

• Language: English
• Title: Synthesis of ethylurea derivates of benzothiazole-2-amine as inhibitors of bacterial topoisomerases

Abstract

In the experimental work we synthesized ethylurea derivatives of benzothiazole-2-amine, which differed in substituents attached at position 6. The purpose of different substituents was improving solubility of designed compounds and forming interactions with amino-acid residues Arg76 and Arg136, because they are crucial to achieve good inhibition. The structure and the purity of synthesized compounds were tested with chromatographic and spectroscopic techniques and evaluated for potential inhibitory activity on isolated enzyme DNA gyrase from bacterial species Escherichia coli (E. coli).

• Keywords: bacterial resistance, DNA gyrase, ethylurea derivatives, inhibitors