Bioactive Molecules via Morita–Baylis–Hillman Chemistry

Abstract Morita–Baylis–Hillman (MBH) chemistry was applied to the synthesis of a variety of new chemical entities and their bioactivity was evaluated. Various substances synthesized via MBH chemistry have: antimalarial, anti-inflammatory, antidiabetic, antimicrobial, antitubercular, and anticancer activity and also act as phosphodiesterase inhibitors. There are a few instances animal model and biology studies explored. Several hits and lead molecules are identified and their IC50 values listed. The simplicity of Morita–Baylis–Hillman chemistry provides a realistic, impactful option for the pharma industry. 1 Introduction 2 Antimalarial Activity 3 Anti-inflammatory Activity of MBH Adducts Coupled to Heterocycles 4 Antidiabetic Activity of Epalrestat Analogues Derived from MBH Adducts 5 Antimicrobial Activity 6 Antitubercular Activity of N-Cinnamyl-isatins 7 Inhibitors of Phosphodiesterase-3 (PDE3); Cardiotonic Agents 8 Anticancer Activity 9 Asymmetric Morita–Baylis–Hillman Reactions 10 Conclusion