Medicinal Chemistry in Animal Health and the Unique Challenges
Dr. Matthew Bedore
Medicinal chemistry in human health is a well-documented discipline but the challenges facing an animal health medicinal chemist are often less known and can vary from their human health counterpart. One such example is in heartworm (Dirofilaria immitis) prevention in companion animals which is becoming increasingly problematic due to developing resistance against current macrocyclic lactone (ML) treatments. In order to combat resistance, new substrate is being sought to achieve HW prevention. Depsipeptides, such as emodepside, represent an exciting class of molecules which have shown efficacy against ML resistant heartworm strains in dogs. Initial structure-activity relationship development and navigation of complex synthetic challenges led to the identification of new depsipeptides with improved in vitro potency and larval stage selectivity over emodepside. The unique challenges of this class of compounds for treating canine heartworm disease and the overall differences in early discovery for animal health will be discussed from a medicinal chemistry perspective.