The blurring line between small molecules and peptides as pharmaceuticals is a function of the changed landscape of therapeutic targets, improvements in drug delivery technology and frankly, the collapse of certain dogmatic rules that have been misapplied in drug discovery.
The result of this has been a resurgence in the need to apply organic synthesis techniques that efficiently produce bioactive molecules through multistep processes without the burdens of extensive purification at each step. In this presentation, I will describe some of the non-amide bond forming reactions that we have utilised in our drug discovery projects, that have yielded exciting leads at GPCRs, anti-viral targets and compounds that facilitate targeted protein degradation.