Alan Joseph Hennessy

TL;DR: This work provides new insights into the mechanism of topoisomerase action and a platform for structure-based drug design of a new class of antibacterial agents against a clinically proven, but conformationally flexible, enzyme class.

TL;DR: The addition of Grignard reagents or organolithium reagents to the SO2-surrogate DABSO generates a diverse set of metal sulfinates, suitable for direct conversion to sulfone products.

TL;DR: X-ray crystallographic studies were used to provide insight into the structural basis for the difference in antibacterial potency between enantiomers and advanced studies were reported on compound 1 which demonstrates good PK and in vivo efficacy properties.

TL;DR: The synthesis of a range of highly functionalized peptidomimetic macrocycles has been accomplished using ring-cl closing metathesis and enyne tandem cross-metathesis-ring-closing metatheses reactions, giving access to rigidified macrocycles modeled on the structures of cyclic peptides and designed to be biologically stable.

TL;DR: The gold-catalysed double functionalisation of indoles is presented, and good yields for the formation of medicinally relevant [6,5,7]-tricyclic indoles are realised.