Abstract: Increasing microbial burden and the development of antimicrobial resistance (AMR) pose a major threat to human health worldwide. In addition to the increased risk of patient death, AMR results in longer hospital stays and increased healthcare costs. This situation is of course undesirable and the most advantageous is the design of new agents with a new/innovative mechanism of action. One possibility for the design of new drugs is inspiration from natural compounds with multiple activities, such as salicylic acid derivatives. By modifying the scaffolds of such compounds, molecules with a broad spectrum of action can be obtained, and therefore it is advantageous to use them for the design of multi-targeted anti-invasive agents. Salicylanilides are simple, small and relatively old molecules, yet they surprise with a wide range of biological activities and the ability to influence various cell structures. Hydroxynaphthalenecarboxanilides can be considered as cyclic analogues of salicylanilides and have also been described mainly for their anti-invasive activity against both cancer lines and Gram-positive bacteria and mycobacteria. Recently, novel anilides structurally derived from the salicylic scaffold have been designed, which showed potent bactericidal activity against clinical isolates of drug-resistant Gram-positive bacteria, as well as activity against mycobacteria. These small molecules will be discussed in this contribution.

Keywords: salicylanilides, hydroxynaphthelene-carboxamides, multi-target drugs, antimicrobial agents

Acknowledgements: This study was supported by projects APVV-22-0133 and VEGA 1/0116/22.

Biography: Josef Jampilek completed his Ph.D. degree in Medicinal Chemistry at the Faculty of Pharmacy of the Charles University (Czech Republic) in 2004. In 2004-2011, he worked in expert and managerial posts in the R&D Division of the pharmaceutical company Zentiva (Czech Republic). Prof. Jampilek deepened his professional knowledge at the Medicinal Chemistry Institute of the Heidelberg University (Germany) and at multiple specialized courses. In 2017, he was designated as a Full Professor of Medicinal Chemistry. At present he works at the Faculty of Natural Sciences of the Comenius University in Bratislava (Slovakia) and the Faculty of Science of the Palacky University in Olomouc (Czech Republic). In addition, he is a visiting professor at the University of Silesia in Katowice (Poland), Cracow University of Technology (Poland) and Hong Kong Baptist University (Hong Kong SAR, China) and an invited professor/expert at various higher educational institutions. He is an author/co-author of more than 35 patents/patent applications, more than 260 peer-reviewed scientific publications, 7 university textbooks, more than 50 chapters in monographs, and many invited lectures at international conferences and workshops. He also received several awards for his scientific results, e.g., from Aventis, Elsevier, Willey, Sanofi and FDA. Prof. Jampílek is also an editor, guest editor and member of the editorial boards of several renowned international scientific journals. Scientific fields of prof. Jampilek are drug design, medicinal chemistry, chemical biology as well as drug delivery nanosystems. The research interests of Prof. Jampilek include design, synthesis, and structure-activity relationships of heterocyclic compounds as anti-infectious, antiproliferative and anti-inflammatory agents as well as agrochemicals. He is also interested in ADME, drug bioavailability and solid-state pharmaceutical analysis.