Drug resistance is a major problem. Here, I consider the mechanisms of action of two classes of drugs/drug leads: the anti-tuberculosis drug SQ-109 and its analogs, and members of the bisamidine class of anti-infectives. Both have multiple sites of action and I will present several crystallographic structures, as well as presenting growth inhibition results against a very broad range of infectious organisms. The results indicate that: multiple-site targeting is responsible for the difficulty in generating resistance to these drugs in bacteria; other organisms are susceptible, due to multi-site targeting, and that combination therapies utilizing such poly-pharmaceuticals offer one route to resistance-resistant therapeutics.Supported by NIH AI074233, GM065367 and CA158191, and by the American Heart Association, Midwest Affiliate

Drug resistance: Multisite targeting of some new drug leads

246th National Meeting (2013)

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