Small Molecules

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For centuries nature has been the only source of biologically active compound. Drawing inspiration from nature and using the principles of organic synthesis and medicinal chemistry we seek to synthesis molecules with intriguing antimicrobial and anticancer activities.

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1) Synthesis of phenazines. The phenazines are heterocycles isolated from bacteria.  They are some of the oldest isolated antibiotics.  However, this family of molecules have shown promise in the treatment of cancer or as antioxidants.  Our group seeks to synthesize phenazine natural products and then use the prepared molecules as scaffolds to build molecular libraries.  Currently, we are working on the development of phenazine antibacterials against the ESKAPE pathogens.   We have recently reported the synthesis and biological evaluation of Endophenazine G and some of its analogues. We are preparing various phenazine molecules to establish structure-activity relationships.

https://www.sciencedirect.com/science/article/abs/pii/S0223523416308157

https://www.sciencedirect.com/science/article/abs/pii/S0223523417309212

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2) Optimization of Citropin 1.1. Natural peptides are intriguing alternatives to traditional antibiotics.  Their mechanism of action is usually associated with membrane disruption.  However, peptides have some limitations including low bioavailability, cell toxicity, and sensitivity to proteolytic enzymes.  We are exploring the effect than unnatural amino acids and peptoids have on Citropin 1.1 activity.

https://www.sciencedirect.com/science/article/abs/pii/S019697811930097X

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3) Chlamydial antibiotics:  Chlamydial infections are a common sexually transmitted bacterial disease in the world. We are developing compounds that can dis-regulate chlamydial proteases.  This will affect metabolic processes killing the pathogen. We are also collaborating with Dr. Scot Oullette to understand the biology of this pathogen.

https://jb.asm.org/content/201/2/e00635-18.abstract

https://pubs.acs.org/doi/abs/10.1021/acs.jmedchem.0c00371

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4) Synthesis of new topoisomerase inhibitors. Coming soon

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5) Synthesis of Curcumin analogues.  Coming Soon