Bioactive Molecules via Morita–Baylis–Hillman Chemistry

Abstract

AbstractMorita–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 Introduction2 Antimalarial Activity3 Anti-inflammatory Activity of MBH Adducts Coupled to Heterocycles4 Antidiabetic Activity of Epalrestat Analogues Derived from MBH Adducts5 Antimicrobial Activity6 Antitubercular Activity of N-Cinnamyl-isatins7 Inhibitors of Phosphodiesterase-3 (PDE3); Cardiotonic Agents8 Anticancer Activity9 Asymmetric Morita–Baylis–Hillman Reactions10 Conclusion