Návrh, syntéza a hodnocení derivátů pyrazinamidu obsahujících 1,2,3-triazolový Iinker jako inhibitorů prolyl-tRNA syntetázy

Puchírová, Dominika

(ENG) Charles University Faculty of Pharmacy in Hradec Králové Department of Pharmaceutical Chemistry and Pharmaceutical Analysis Researcher: Dominika Puchírová Thesis supervisor: doc. PharmDr. Jan Zitko, Ph.D. Consultant: Mgr. Andrea Bachtíková Title of thesis: Synthesis and evaluation of pyrazinamide-containing derivatives 1,2,3-triazole linker as an inhibitor of prolyl-tRNA synthetase This thesis focuses on the design, development and synthesis of novel compounds with potential antimycobacterial activity, while the target structure is mycobacterial prolyl-tRNA synthetase, an enzyme essential for proteosynthesis, growth and cell viability. Basic structure of the proposed compounds is based on previously published 3-aminopyrazinamides with confirmed antimycobacterial activity, with the amide bond partially replaced by 1,2,3-triazole linker in order to increase the affinity for prolyl-tRNA synthetase and thus biological efficacy. The basic structure of the molecules of pyrazinamide with a 1,2,3-triazole linker and simple substituents at aromatic core. Basic structure of pyrazinamide compounds with a 1,2,3-triazole linker and simple substituents on the aromatic core Structural modifications were designed using in silico molecular modeling methods. The synthesis of the resulting compounds was carried...

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