Harnessing medicinal chemistry for sustainable drugs

Lecture held by Dr Maria Laura Bolognesi, Professor of Medicinal Chemistry, University of Bologna, Italy.

Drug discovery is an increasingly complex endeavour, with an always greater cost and a lower efficiency. This is particularly pressing in the area of neglected tropical diseases, where the inadequacy of available treatments, in terms of low access, high toxicity and complicated dosing regimens, calls for efforts focused on sustainable principles. In addition, the concepts of "Green chemistry" and "One health" are gaining momentum and being implemented in the daily practice. For these reasons, as medicinal chemists, we have been motivated not only to develop more appropriate drugs to combat these diseases, but also to do so in a sustainable manner and for potential use in low- and middle-income countries [1]. An enlightening perspective is to use agroindustrial wastes as starting material for the synthesis of novel biologically active compounds, which can then be optimised into novel drugs [2]. With this motivation, we have recently explored the possibility of developing new pharmacological tools from cashew nut shell liquid (CNSL). By using an inexpensive and inedible biowaste as a starting material, these tools are inherently benign by design. In addition, they can be more affordable and accessible to those in need. In this talk, we will present these ideas and discuss our developments in the field [3-5].

[1] Bolognesi, M.L. Chapter Six - Sustainable anti-trypanosomatid drugs: An aspirational goal for medicinal chemistry. In: Annual Reports in Medicinal Chemistry, Academic Press, Editor(s): Kelly Chibale, Volume 52, 2019, pp 153-176; Martinengo B. et al. Harnessing the 12 Green Chemistry Principles for Sustainable Antiparasitic Drugs: Toward the One Health Approach. ACS Infect Dis. 2024 Jun 14;10(6):1856-1870.

[2] Espro, C. et al. Sustainable production of pharmaceutical, nutraceutical and bioactive compounds from biomass and waste. Chem Soc Rev (2021), 50, 11191-11207.

[3] Cerone, M. et al. Discovery of Sustainable Drugs for Neglected Tropical Diseases: Cashew Nut Shell Liquid (CNSL)‐Based Hybrids Target Mitochondrial Function and ATP Production in Trypanosoma Brucei. ChemMedChem (2019) 14, 621-635.

[4] Nunes Lemes L.F. et al. Valorizing constituents of cashew nut shell liquid towards the sustainable development of new drugs against Chagas disease. ACS Infect. Dis. (2023), 9, 1334–1345.

[5] Rossi M. et al. Benign-by-Design SAHA Analogues for Human and Animal Vector-Borne Parasitic Diseases. ACS Med Chem Lett Article ASAP DOI: 10.1021/acsmedchemlett.4c00242

Maria Laura Bolognesi is Professor of Medicinal Chemistry and Coordinator of the Biotechnological, Biocomputational, Pharmaceutical and Pharmacological Sciences PhD Program at the University of Bologna, Italy, and Associate Editor at the Journal of Medicinal Chemistry. 

The lecture is organized by Professor Trond Ulven, Department of Drug Design and Pharmacology, Faculty of Health and Medical Sciences, University of Copenhagen.

The lecture is free of charge and open for attendance by all interested parties. It is not necessary to pre-register.