Syngenta Crop Protection AG, Switzerland
Posters & Accepted Abstracts: Med Chem (Los Angeles)
Worldwide, fungal infections take more than 1.3 million lives each year. In addition, over 300 million people are affected by a serious fungal infection. Three classes of antifungals are mainly used to manage these types of invasive fungal infection. The over-reliance on the same medicines acting on a limited number of modes of action has induced a selection pressure amongst the originally susceptible pathogens. As a consequence, drug resistance has become increasingly common and has diminished the arsenal of effective antifungal drugs. Furthermore, some drugs have additional significant limitations. For example, echinocandins need to be administrated intravenously due to their poor oral bioavailability, and amphotericin B has been known to induce adverse nephrotoxicity. This clearly shows the strong need for new molecules which are able to control pathogens showing resistance to our current antifungal products. To bring new antifungals into development, researchers first need to identify new lead molecules. In order to achieve this, they often rely on screening techniques, with phenotypic screening of new compounds being the most preferred. In this presentation, learning├ó┬?┬?s from several years of research and surveys of the antifungal literature will be shared: unwanted compounds not only adversely affect enzyme assays (figure 1) but also phenotypic screens and hits, as a consequence needs to be selected very carefully. In addition, we would like to share examples of what we believe are good hits for antifungal research but that we were not able to pursue further due to resource limitations. We hope that this will encourage scientists to take some of them forward and help to tackle the global challenge of antifungal research.
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