Abstract: Multi-target drug discovery represents an innovative approach of medicinal chemistry to overcoming a crisis in drug design, especially of anti-invasive drugs, reflected in the small number of newly approved drugs. This approach is based on the concepts of privileged scaffolds, polypharmacology and multifactorial diseases. Thus it seems to be a very useful tool in the design of antineoplastic and anti-infectious agents, as therapeutic agents designed in this way interact with multiple targets and thus prevent resistance, acting against various classes of pathogens and simultaneously against tumor cells. Similarly, multi-target drugs can be designed for the simultaneous treatment of autoimmune, inflammatory and invasive diseases. This contribution is focused especially on the investigation of new ring-substituted cinnamic acid-based compounds with estimated antimicrobial and anti-inflammatory activity. Structure-activity relationships and the supposed mechanism of action are discussed.

Keywords: multi-target compounds, privileged scaffolds, cinnamic acid

Acknowledgements: This study was supported by the Slovak Research and Development Agency (Grant No. APVV-17-0373).

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 2009, he became an Associate Professor of Medicinal Chemistry at the Faculty of Pharmacy of the University of Veterinary and Pharmaceutical Sciences Brno (Czech Republic). In 2017, he became a Full Professor of Medicinal Chemistry at the Faculty of Pharmacy of the Comenius University (Slovakia). He is an author/co-author of more than 30 patents/patent applications, more than 200 peer-reviewed scientific publications, 7 university textbooks, more than 30 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. 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 photosynthesis inhibitors. He is also interested in ADME, drug bioavailability and solid-state pharmaceutical analysis.