Hydroxyazoles as acid isosteres and their drug design applications—Part 2: Bicyclic systems

Hydroxyazoles are acidic systems that are considered isosteres of the carboxylic acid group; because of their efficacy in exploring chemical space, they are considered an efficient bioisosteric tool for designing optimized compounds with added IP value. Recently, we and other groups applied such systems in the framework of hit-to-lead optimization processes. Having already covered in this volume (Sainas et al., 2020) the chemo-physical properties, synthetic methodologies and drug design application of monocyclic hydroxyazoles, in this chapter we complete the scenario focusing on the parent bicyclic hydroxyazole systems.