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Silicon-Containing Building Blocks for Drug Design

Silicon-containing compounds have been largely ignored in drug design until recently. Silicon can be considered a bioisostere of carbon and hence offers an innovative avenue in drug discovery. For example, C/Si exchange in drug-like scaffolds provides an exciting approach in medicinal chemistry to improve ADME/Tox profile and to enhance potency of the biologically active compounds. Herein we have designed and synthesized a library of silicon-containing building blocks for drug design.

Case studies

Advantages of “Silicon Switch”:

  • Bond length C–C = 1.54 Å, C–Si = 1.87 Å → changes in the interactions with specific proteins;
  • Increase in lipophilicity;
  • Si prefers higher coordination numbers → access to compounds for which corresponding carbon analogs are not available.

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More than 30 of silicon-containing building blocks from stock on a 5-10 g scale.

MedChem Highlights

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