Next Article in Journal
Discrimination of Natural Mature Acacia Honey Based on Multi-Physicochemical Parameters Combined with Chemometric Analysis
Previous Article in Journal
Anti-Diabetic Effect of a Shihunine-Rich Extract of Dendrobium loddigesii on 3T3-L1 Cells and db/db Mice by Up-Regulating AMPK–GLUT4–PPARα
Due to scheduled maintenance work on our core network, there may be short service disruptions on this website between 16:00 and 16:30 CEST on September 25th.
Article

New and Potent Quinuclidine-Based Antimicrobial Agents

1
Department of Chemistry, Faculty of Science, University of Zagreb, Horvatovac 102a, HR-10000 Zagreb, Croatia
2
Department of Chemistry, Faculty of Science, University of Split, R. Boškovića 33, HR-21000 Split, Croatia
3
KB “Sestre milosrdnice”, Vinogradska cesta 29, HR-10000 Zagreb, Croatia
4
Institut Ruđer Bošković, Bijenička cesta 54, HR-10000 Zagreb, Croatia
5
Department of Biology, Faculty of Science, University of Split, R. Boškovića 33, HR-21000 Split, Croatia
*
Authors to whom correspondence should be addressed.
Molecules 2019, 24(14), 2675; https://doi.org/10.3390/molecules24142675
Received: 9 June 2019 / Revised: 13 July 2019 / Accepted: 18 July 2019 / Published: 23 July 2019
Developing new antibiotics is currently very important since antibiotic resistance is one of the biggest problems of global health today. In the search for a new class of potential antimicrobial agents, ten new compounds were designed and synthesized based on the quinuclidinium heterocyclic core and the oxime functional group. The antimicrobial activity was assessed against a panel of representative gram-positive and gram-negative bacteria. All compounds demonstrated potent activity against the tested microorganisms, with the minimum inhibitory concentration (MIC) values ranging from 0.25 to 256.00 μg/mL. Among the tested compounds, two quaternary compounds, para-N-chlorobenzyl and meta-N-bromobenzyl quinuclidinium oximes, displayed the most potent and broad-spectrum activity against both gram-positive and gram-negative bacterial strains (MIC values from 0.25 to 4.00 μg/mL), with the lowest value for the important multidrug resistant gram-negative pathogen Pseudomonas aeruginosa. In the case of Klebsiella pneumoniae, activity of those compounds are 256-fold and 16-fold better than gentamicin, respectively. MTT assays showed that compounds are nontoxic for human cell lines. Multi-way analysis was used to separately reduce dimensionality of quantum chemical data and biological activity data to obtain a regression model and the required parameters for the enhancement of biological activity. View Full-Text
Keywords: antimicrobial potency; quinuclidinium oximes; gram-positive and gram-negative bacteria; multi-way analysis antimicrobial potency; quinuclidinium oximes; gram-positive and gram-negative bacteria; multi-way analysis
Show Figures

Figure 1

MDPI and ACS Style

Radman Kastelic, A.; Odžak, R.; Pezdirc, I.; Sović, K.; Hrenar, T.; Čipak Gašparović, A.; Skočibušić, M.; Primožič, I. New and Potent Quinuclidine-Based Antimicrobial Agents. Molecules 2019, 24, 2675. https://doi.org/10.3390/molecules24142675

AMA Style

Radman Kastelic A, Odžak R, Pezdirc I, Sović K, Hrenar T, Čipak Gašparović A, Skočibušić M, Primožič I. New and Potent Quinuclidine-Based Antimicrobial Agents. Molecules. 2019; 24(14):2675. https://doi.org/10.3390/molecules24142675

Chicago/Turabian Style

Radman Kastelic, Andreja, Renata Odžak, Iskra Pezdirc, Karlo Sović, Tomica Hrenar, Ana Čipak Gašparović, Mirjana Skočibušić, and Ines Primožič. 2019. "New and Potent Quinuclidine-Based Antimicrobial Agents" Molecules 24, no. 14: 2675. https://doi.org/10.3390/molecules24142675

Find Other Styles
Note that from the first issue of 2016, MDPI journals use article numbers instead of page numbers. See further details here.

Article Access Map by Country/Region

1
Back to TopTop