Australian Journal of Chemistry is approaching its eighth decade of publishing key work across many spheres of chemistry, both national and international. As the current co-editors-in-chief, we are delighted to introduce this special virtual issue of the journal that highlights a selection of the finest recent articles in medicinal chemistry. The subject itself is diverse and principally addresses drug discovery including of natural products and new methodologies for the synthesis of bioactive compounds to the pharmacokinetics and pharmacodynamics of new drugs. In this collection of ten articles from recent issues of the journal, the breadth and excellence of Australasian medicinal chemistry is highlighted. It ranges from the preparation of plant-derived cyclic peptides as drug design scaffolds, the development of β-, γ-, or δ-thiol ligation auxiliaries of the ligation–desulfurization reactions, isolation of novel cytotoxic terpenes from the Australian nudibranch Goniobranchus splendidus to ring-closing metathesis and CuI-catalyzed azide–alkyne cycloaddition for the preparation of macrocycles, and the synthesis of the naturally occurring cyclic peptide lassomycin. We are proud to also highlight the significant contributions to medicinal chemistry research made by several outstanding women researchers. We hope you enjoy this special issue as much as we do!
John Wade and George Koutsantonis