Chiral Isochalcogenourea Lewis Base Organocatalysis
Mario Waser
Johannes Kepler University Linz,  Austria

Abstract:
Chiral Isochalcogenoureas (IChU) are versatile Lewis base (LBs) organocatalysts that allow for numerous highly enantioselective transformations. Over the last years our group had a strong interest in the utilization of these chiral LBs for the covalent activation, control and utilization of simple carboxylic acid derivatives (via in situ C1 ammonium enolate formation) and allenoates (via in situ betaine formation).Furthermore, we are also interested in the design and use of new catalyst derivatives and in the elucidation of their key properties such as nucleophilicity and basicity. In this presentation I will give an overview of our most recent results focusing on the development and mechanistic understanding of new catalysts and new transformations.

Selected recent contributions related to this topic:
  - M. Piringer, A. Scheucher, M. Hofer, M. Bechmann, A. R. Ofial, L. Stockhammer, Mario Waser ChemistryEurope., 2026, 4, e202500443.
  - L. Stockhammer, K. Kasten, A. Eitzinger, L. S. Vogl, M. Piringer, D. Weinzierl, A. R. Ofial, A. D. Smith, Mario Waser Angew. Chem. Int. Ed., 2025, 64, e202514865.
  - Lukas S. Vogl, Peter Mayer, Raphael Robiette, Mario Waser Angew. Chem. Int. Ed., 2024, 63, e202315345.
  - Magdalena Piringer, Mario Hofer, Lukas S. Vogl, Peter Mayer, Mario Waser Adv. Synth. Catal. 2024, 366, 2115-2122.
  - David Weinzierl, Magdalena Piringer, Paul Zebrowski, Lotte Stockhammer, Mario Waser Org. Lett., 2023, 25, 3126-3130.
  - Lotte Stockhammer, Rebecca Craik, Uwe Monkowius, David B. Cordes, Andrew D. Smith, Mario Waser ChemistryEurope, 2023, 1, e202300015

Multi-target Anti-infectives Based on Quinoline Scaffolds
Josef Jampilek
1. Palacky University Olomouc, Czech Republic;
2. University of Silesia, Poland

Abstract:
Multi-target agents are chemical entities designed to interact with two or more biological targets that are crucial for the mechanism or progression of a disease. This innovative strategy contrasts with the traditional “one drug, one target” paradigm of drug discovery. This approach is based on the concepts of privileged structures, polypharmacology, and multifactorial diseases. It appears to be a generally useful tool in the design of anti-invasive (anti-infective, anti-cancer) drugs, as the therapeutic agents designed in this way interact with multiple targets, so that they are able to destroy both sensitive and resistant pathogens/cells while also preventing their emergence. Multi-target anti-infectives thus represent compounds resistant to resistance.

In modern molecular architecture, heterocyclic systems represent privileged scaffolds. According to statics, heterocycles constitute more than 85% of biologically active molecules. This phenomenon is not accidental; heterocycles provide an ideal balance between the rigidity necessary for molecular recognition and the chemical diversity that allows interactions with a wide range of biological targets.

Quinoline-based compounds have various promising biological properties and therefore have received special attention in the field of drug design and medicinal chemistry. The quinoline scaffold can be easily and rapidly synthesized and functionalized, which indicates the importance of this privileged structure. Moreover, this simple structural element has unique physicochemical properties and allows for a large number of target- or diversity-oriented modifications.

This contribution focuses on the investigation of ring-substituted hydroxy- and aminoquinolines and their antifungal, antibacterial, antimycobacterial and antiprotozoal activities.