Autor: Brulíková, L.; Šlachtová, V.; Šebela, M.; Cappoen, D.
Název práce v češtině: Syntéza novych inhibitorů mykobakteriální Zmp1
Název práce v angličtině: Synthesis of novel mycobacterial Zmp1 inhibitors
Klíčová slova v češtině: Zmp1, Mycobacterium tuberculosis, thiazolidinediony, hydroxamáty, MALDI-TOF
Klíčová slova v angličtině:Zmp1, Mycobacterium tuberculosis, thiazolidinediones, hydroxamates, MALDI-TOF
Abstrakt česky: Zinc metalloprotease 1 (Zmp1) is an extracellular enzyme, which has been found essential for the intracellular survival and pathogenesis of Mycobacterium tuberculosis.1 Zmp1 and its inhibition leading to virulence attenuation may represent a potentially useful drug target in the treatment of tuberculosis.
In this work, we have developed an efficient synthetic protocol for the preparation of a series of thiazolidinedione-hydroxamates and assessed their inhibitory properties towards a recombinant Zmp1 from Mycobacterium tuberculosis by MALDI-TOF MS. This characterization was completed by whole-cell biological activity and cytotoxicity tests. Nine of the tested compounds were found to inhibit the enzymatic reaction more effectively than the generic metalloprotease inhibitor phosphoramidon.
Abstrakt anglicky: Zinc metalloprotease 1 (Zmp1) is an extracellular enzyme, which has been found essential for the intracellular survival and pathogenesis of Mycobacterium tuberculosis.1 Zmp1 and its inhibition leading to virulence attenuation may represent a potentially useful drug target in the treatment of tuberculosis.
In this work, we have developed an efficient synthetic protocol for the preparation of a series of thiazolidinedione-hydroxamates and assessed their inhibitory properties towards a recombinant Zmp1 from Mycobacterium tuberculosis by MALDI-TOF MS. This characterization was completed by whole-cell biological activity and cytotoxicity tests. Nine of the tested compounds were found to inhibit the enzymatic reaction more effectively than the generic metalloprotease inhibitor phosphoramidon.
Jazyk v originále: angličtina
Publikace abstraktu: sborník, 45
Forma prezentace: přednáška
Název konference: 18th Blue Danube Symposium on Heterocyclic Chemistry
Místo konání: Ljublan, Slovinsko
Datum konání: september 18 – 21
Rok konání: 2019
Způsob financování: JG_2019_002