Small molecule design strategies for probing structure-activity relationships: bacterial virulence modulation via CpxRA, the total synthesis of Picrasma alkaloids, and coronavirus main protease inhibitors

Abstract

The overall aim of this work is to contribute to molecular design strategies for early lead development while probing structure-activity relationships via the design and synthesis of small molecules. This dissertation will tell three distinct stories: (1) exploitation of CpxRA as a target for virulence modulation in Gram-negative bacteria, (2) work towards the total synthesis of Picrasidine natural product family members, and (3) the rational design and synthesis of SARS-CoV-2 main protease inhibitors.