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Hetero[3.1.1]propellanes – Precursors to novel, versatile meta-bioisosteres for enhanced drug discovery

Image from Licence Details: Hetero[3.1.1]propellanes – Precursors to novel, versatile meta-bioisosteres for enhanced drug discovery

Applications: Drug discovery, lead optimisation, SAR studies

Features Benefits
  • Novel heteroatom-containing [3.1.1] propellanes offer an entry to compact hetero-bicyclo[3.1.1]heptanes for precise spatial control of substituents
  • Potential to improve drug properties e.g. enhance solubility, optimise lipophilicity
  • Bioisosteric design mimics meta-substituted benzene and pyridine motifs
  • Expands the chemical space, enabling access to novel 3D fragments for better target engagement and selectivity
  • General synthetic route enables broad substitution patterns and heteroatom variants
  • Quickly generates diverse range of analogues for structure–activity relationship studies
  • Efficient single-step bridgehead disubstitution
  • Simplifies synthesis of structurally complex hetero-BCHeps with broad therapeutic applicability
  • Hetero-BCHep products are isolable, storable and compatible with downstream transformations
  • Reduces development risk by replacing problematic aromatic rings with robust, predictable scaffolds

Patented & available for:

  • Licensing
  • Co-development
  • Consulting
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