Pregled bibliografske jedinice broj: 1141906
Amido-quinuclidine based QACs as a new soft antimicrobial agents susceptible to protease degradation
Amido-quinuclidine based QACs as a new soft antimicrobial agents susceptible to protease degradation // Book of abstracts
Basel, Švicarska, 2021. str. 420-420 (poster, međunarodna recenzija, sažetak, znanstveni)
CROSBI ID: 1141906 Za ispravke kontaktirajte CROSBI podršku putem web obrasca
Naslov
Amido-quinuclidine based QACs as a new soft
antimicrobial agents susceptible to protease
degradation
Autori
Crnčević, Doris ; Odžak, Renata ; Šprung, Matilda
Vrsta, podvrsta i kategorija rada
Sažeci sa skupova, sažetak, znanstveni
Izvornik
Book of abstracts
/ - , 2021, 420-420
Skup
XXVI EFMC International Symposium on Medicinal Chemistry
Mjesto i datum
Basel, Švicarska, 29.08.2021. - 02.09.2021
Vrsta sudjelovanja
Poster
Vrsta recenzije
Međunarodna recenzija
Ključne riječi
synthesis, quaternary ammonium compounds (QACs), amide bond, biological activity
Sažetak
Quaternary ammonium compounds (QACs) are biologically active amphiphiles displaying potent antimicrobial properties (M.D. Joyce et al., 2015). Given the alarming number of QACs resistant environmental isolates, the aim of further QACs research is to synthetise soft QACs variants more prone to either spontanious or enzymatic degradation. Our previous studies on QACs have shown that quinuclidine is a good starting structure for quaternization and that its derivatives have potent antimicrobial activity (Bazina et al., 2019). It is also known that amide bond is susceptible to peptidase degradation. This fact implies that compounds containing such bond could be degraded more easily in the environment by enzymatic decomposition. For these reasons, we were set to synthesize new amido-quinuclidine derivatives with long alkyl chains to yield biologically active and more environmental friendly QACs variants. A series of six new compounds QAd12, MeQAd12, AlyQAd12, QAd14, MeQAd14 and AlyQAd14 were synthesized and analyzed for their antimicrobial activity using a panel of pahtogenic bacteria and fungus. All compounds display good antimicrobial potential at concentrations in μM range. To investigate if those compounds are succesfully degraded by cellular peptidases, enzymatic digestion of compounds using cell lysates will be preformed. This finding might shed light on new potential mechanism for production of environmental friendly QACs.
Izvorni jezik
Engleski
Znanstvena područja
Kemija
POVEZANOST RADA
Projekti:
HRZZ-UIP-2020-02-2356 - Otkriće i razvoj novih biološki aktivnih kvaternih amonijevih spojeva derivata kinuklidina (QACBioAct) (Šprung, Matilda, HRZZ ) ( CroRIS)
Ustanove:
Prirodoslovno-matematički fakultet, Split