Discovery of New Antimicrobial Agents using Combinatorial Chemistry

Combinatorial chemistry has become an important aspect of medicinal research due to its flexibility and the ability to produce large numbers of potential therapeutic agents. Once compounds are made, they must be screened to determine if there is any biological activity. This research project focused on developing a screening method for chemical agents produced by a graduate student in the chemistry department at Wright State University. After an acceptable screening method was found, the goal of the project was to determine if compounds produced had either antibacterial activity, antifungal activity, or both. Seven compounds exhibited biological activity. Two of these compounds had activity against all organisms tested. Five compounds had activity against only Staphylococcus aureus. Also, initial toxicity studies were performed on the two compounds that had activity against both bacteria and fungi. The toxicity was detected by cytopathic effect (CPE) noted in human and monkey cell lines. One compound demonstrated severe toxicity while the other compound demonstrated slight toxicity. Additional research, including animal safety studies, will be required to determine if these compounds are viable prospects for development into antimicrobial agents. This research confirmed that it is possible to use combinatorial methods to produce agents. However, the ability to produce antimicrobial compounds is only a small part of producing a useful drug