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Pregled bibliografske jedinice broj: 1161320

Synthesis and antibacterial activities of new amidoquinuclidines and their quaternary salts


Crnčević, Doris; Sabljić, Antonio; Odžak, Renata; Šprung, Matilda
Synthesis and antibacterial activities of new amidoquinuclidines and their quaternary salts // Book of Abstracts
Zagreb, Hrvatska, 2021. str. 11-11 (predavanje, domaća recenzija, sažetak, znanstveni)


CROSBI ID: 1161320 Za ispravke kontaktirajte CROSBI podršku putem web obrasca

Naslov
Synthesis and antibacterial activities of new amidoquinuclidines and their quaternary salts

Autori
Crnčević, Doris ; Sabljić, Antonio ; Odžak, Renata ; Šprung, Matilda

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

Izvornik
Book of Abstracts / - , 2021, 11-11

Skup
5th Mini Symposium of Section of Medicinal and Pharmaceutical Chemistry

Mjesto i datum
Zagreb, Hrvatska, 30.11.2021

Vrsta sudjelovanja
Predavanje

Vrsta recenzije
Domaća recenzija

Ključne riječi
Synthesis, quaternary ammonium compounds, amidoquinuclidines, biological activity, protease degradation

Sažetak
In recent years, the demand for development of new and more effective antiseptics and disinfectants has risen. One reason for this is the COVID-19 pandemic and the widespread use of these formulations provoking higher incidence of bacterial resistance in future years [1]. Quaternary ammonium compounds (QACs) have been shown to be effective antimicrobial candidates that tend to disrupt the bacterial membrane, leading to leakage of cytoplasm and subsequent cell lysis [2]. We and others have shown that natural products could be used as chemical scaffolds for quaternization to yield QACs of potent antimicrobial activities [3, 4]. Here we report the new series of such natural scaffold- guided structures containing amide bond as a potential substrate for protease degradation. The introduction of amide bond might result in biodegradable QACs, hence variants that have much shorter lifetime in the environment. The 3- aminoquinuclidine was substituted with alkyl chains of different length (10, 12 and 14 C-atoms) to yield precursors for quaternization (Figure 1). The quaternization was performed with appropriate alkyl halide reagents to obtain amidoquinuclidine QACs in good yields (Figure 2). The minimum inhibitory concentrations (MICs) were determined for both, amidoquinuclidines and their QACs, against a panel of Gram-positive and Gram-negative bacteria. As expected, the activity of the QACs was significantly better than for corresponding amidoquinuclidines which is in good correlation with calculated lipophilicity coefficients (cLogP). Our results suggest that amidoquinuclidine QACs could be good antibacterial candidates. The future experiments will elucidate weather these candidates are substrates for protease degradation.

Izvorni jezik
Engleski

Znanstvena područja
Kemija

Napomena
Neobjavljeni rad



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

Citiraj ovu publikaciju:

Crnčević, Doris; Sabljić, Antonio; Odžak, Renata; Šprung, Matilda
Synthesis and antibacterial activities of new amidoquinuclidines and their quaternary salts // Book of Abstracts
Zagreb, Hrvatska, 2021. str. 11-11 (predavanje, domaća recenzija, sažetak, znanstveni)
Crnčević, D., Sabljić, A., Odžak, R. & Šprung, M. (2021) Synthesis and antibacterial activities of new amidoquinuclidines and their quaternary salts. U: Book of Abstracts.
@article{article, author = {Crn\v{c}evi\'{c}, Doris and Sablji\'{c}, Antonio and Od\v{z}ak, Renata and \v{S}prung, Matilda}, year = {2021}, pages = {11-11}, keywords = {Synthesis, quaternary ammonium compounds, amidoquinuclidines, biological activity, protease degradation}, title = {Synthesis and antibacterial activities of new amidoquinuclidines and their quaternary salts}, keyword = {Synthesis, quaternary ammonium compounds, amidoquinuclidines, biological activity, protease degradation}, publisherplace = {Zagreb, Hrvatska} }
@article{article, author = {Crn\v{c}evi\'{c}, Doris and Sablji\'{c}, Antonio and Od\v{z}ak, Renata and \v{S}prung, Matilda}, year = {2021}, pages = {11-11}, keywords = {Synthesis, quaternary ammonium compounds, amidoquinuclidines, biological activity, protease degradation}, title = {Synthesis and antibacterial activities of new amidoquinuclidines and their quaternary salts}, keyword = {Synthesis, quaternary ammonium compounds, amidoquinuclidines, biological activity, protease degradation}, publisherplace = {Zagreb, Hrvatska} }




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