Naslov
Interactions of macrolide antibiotics and macrozones under the scope of NMR

Autori
Novak, Predrag

Vrsta, podvrsta i kategorija rada
Sažeci sa skupova, sažetak, znanstveni

Izvornik
Book of abstracts, EUROMAR 2021 / - , 2021, 48-48

Skup
17th EUROMAR 2021 conference

Mjesto i datum
Portorož, Slovenija, 04.07.2021. - 08.07.2021

Vrsta sudjelovanja
Pozvano predavanje

Vrsta recenzije
Međunarodna recenzija

Ključne riječi
macrolide antibiotics, macrozones, interactions, drug design

Sažetak
Macrolide antibiotics, such as azithromycin have been in clinical use for over 60 years, mostly due to their high efficacy, safety and favourable pharmacokinetics [1]. Macrolides bind to the 23S rRNA of the 50S subunit, near or at the peptidyl transferase center (PTC), block the nascent peptides exit tunnel and thus inhibit the synthesis of bacterial proteins. Multi-drug resistant microbial pathogens compromise their use as effective antimicrobials and poses serious treats to human health worldwide which demand novel and more potent antimicrobial agents to be discovered. An effective approach to overcoming this problem is to understand the principles of how these drugs interact with their biological targets. Macrozones belong to a novel class of azithromycin-thiosemicarbazone conjugates that exhibit very good antibacterial activities against both susceptible and resistant bacterial strains [2]. In this talk results of interaction studies of macrolide antibiotics and some selected macrozones with their biological targets will be presented [2]. A combination of NMR experiments such as transferred nuclear Overhauser effect spectroscopy (trNOESY), saturation transfer difference (STD), diffusion and solvent paramagnetic relaxation experiments (PRE) and molecular modelling has been employed to characterize binding epitopes and asses bound conformations [4, 5]. The data so obtained can serve as a basis for design of novel compounds with an improved biological profile

Izvorni jezik
Engleski

Znanstvena područja
Kemija

POVEZANOST RADA