Carboxylic Acid Bioisosteres in Medicinal Chemistry: Synthesis and Properties

Lead optimization represents the tedious process of fine-tuning lead compounds from biologically active hits to suitable drug candidates for clinical trials. By chemically modifying a hit structure, an improved compound can be obtained in terms activity, selectivity, and pharmacokinetic ADME (absorption, distribution, metabolism, excretion) properties. The carboxylic acid moiety is known crucial functionality many pharmaceutically compounds. Despite its common use as key drugs, presence molecule often associated with poor properties toxicity. In this literature overview, we discuss how shortcomings circumvented by replacing bioisosteres. way, positive aspects moiety, such example, virtue capacity form hydrogen bonds, maintained or even improved. To that end, provide overview most promising bioisosteres selection synthetic routes towards main functionalities.