Current Parallel Solid-Phase Synthesis of Drug-like Oxadiazole and Thiadiazole Derivatives for Combinatorial Chemistry

ACS Comb Sci. 2018 Jun 11;20(6):309-329. doi: 10.1021/acscombsci.8b00044. Epub 2018 May 7.

Abstract

Solid-phase organic synthesis is a powerful tool in the synthesis of small organic molecules and building of libraries of compounds for drug discovery. Heterocyclic compounds are important components of the drug discovery field as well and serve as a core for hundreds of marketed drugs. In particular, oxadiazole and thiadiazole cores are compounds of great interest due to their comprehensive biological activities and structural features. Therefore, a plethora of oxadiazole and thiadiazole synthesis methodologies have been reported to date, including solution and solid-phase synthesis methodologies. In this review, we concentrate on and summarize solid-phase synthetic approaches of the oxadiazole and thiadiazole derivatives.

Keywords: combinatorial chemistry; drug design; oxadiazole; parallel synthesis; solid-phase synthesis; thiadiazole.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Combinatorial Chemistry Techniques
  • Cycloaddition Reaction
  • Drug Design
  • Molecular Structure
  • Oxadiazoles / chemical synthesis*
  • Oxidation-Reduction
  • Small Molecule Libraries / chemical synthesis
  • Solid-Phase Synthesis Techniques / methods
  • Thiadiazoles / chemical synthesis*

Substances

  • Oxadiazoles
  • Small Molecule Libraries
  • Thiadiazoles