Simplified immunosuppressive and neuroprotective agents based on gracilin A.

ABSTRACT: The architecture and bioactivity of natural products frequently serve as embarkation points for the exploration of biologically relevant chemical space. Total synthesis followed by derivative synthesis has historically enabled a deeper understanding of structure-activity relationships. However, synthetic strategies towards a natural product are not always guided by hypotheses regarding the structural features required for bioactivity. Here, we report an approach to natural product total synthesis that we term 'pharmacophore-directed retrosynthesis'. A hypothesized, pharmacophore of a natural product is selected as an early synthetic target and this dictates the retrosynthetic analysis. In an ideal application, sequential increases in the structural complexity of this minimal structure enab

SUBMITTER: Abbasov ME 

PROVIDER: S-EPMC6532426 | biostudies-literature | 2019 Apr

REPOSITORIES: biostudies-literature