Adventures in drug-like chemistry space: from oxetanes to spiroazetidines and beyond

• Published in: Chimia Vol. 68; no. 7-8; p. 492
• Main Authors: Rogers-Evans, Mark, Knust, Henner, Plancher, Jean-Marc, Carreira, Erick M, Wuitschik, George, Burkhard, Johannes, Li, Dong B, Guérot, Carine
• Format: Journal Article
• Language: English
• Published: Switzerland Swiss Chemical Society 01.01.2014
• Subjects: Azetidines - chemical synthesis; Azetidines - chemistry; Chemistry and biology space; Compact modules; Drug Discovery; Ethers, Cyclic - chemical synthesis; Ethers, Cyclic - chemistry; Molecular Structure; Oxetanes; Shape diversity; Spiro Compounds - chemical synthesis; Spiro Compounds - chemistry; Spiroazetidines
• ISSN: 0009-4293; 2673-2424
• DOI: 10.2533/chimia.2014.492

Recently we have documented research efforts aimed at new classes of oxetanes as well as spiroheteroalicyclic ring systems (which we have termed 'Compact Modules') designed to expand the palette of tailored module scaffolds available to medicinal chemists, which constitute an important role for synthetic chemistry in the drug discovery process. An essential component for this process is to provide access to specific molecular topologies with functional group diversity, essential for generating leads that discriminate among biological targets, therefore promoting selectivity and enhancing the safety profile of the final clinical candidates.