Quercetin derivatives: Drug design, development, and biological activities, a review

Eur J Med Chem. 2022 Feb 5:229:114068. doi: 10.1016/j.ejmech.2021.114068. Epub 2021 Dec 24.

Abstract

More studies are needed to develop new drugs for problems associated with drug resistance and unfavorable side effects. The natural flavonoid of quercetin revealed a wide range of biological activities by the modulation of various targets and signaling pathways. However, quercetin's low solubility and poor bioavailability have restricted its applicability; as a result, researchers have attempted to design and synthesize numerous novel quercetin derivatives using various methodologies in order to modify quercetin's constraints; the physico-chemical properties of quercetin's molecular scaffold make it appealing for drug development; low molecular mass and chemical groups are two of these characteristics. Therefore, the biological activities of quercetin derivatives, as well as the relationship between activity and chemical structure and their mechanism of action, were investigated. These quercetin-based molecules could be valuable in the creation and discovery of medications for a number of diseases.

Keywords: Anti-bacterial; Anti-cancer; Anti-inflammatory; Anti-oxidant; Drug design; Quercetin; SAR.

Publication types

  • Review

MeSH terms

  • Animals
  • Anti-Bacterial Agents / chemistry*
  • Anti-Bacterial Agents / pharmacology
  • Antineoplastic Agents / chemistry*
  • Antineoplastic Agents / pharmacology
  • Antioxidants / chemistry*
  • Antioxidants / pharmacology
  • Biological Availability
  • Biological Products / chemistry*
  • Biological Products / pharmacology
  • Drug Design
  • Drug Development
  • Humans
  • Molecular Structure
  • Neuroprotective Agents / chemistry*
  • Neuroprotective Agents / pharmacology
  • Quercetin / chemistry*
  • Quercetin / pharmacology
  • Reactive Oxygen Species / metabolism
  • Signal Transduction
  • Solubility
  • Structure-Activity Relationship

Substances

  • Anti-Bacterial Agents
  • Antineoplastic Agents
  • Antioxidants
  • Biological Products
  • Neuroprotective Agents
  • Reactive Oxygen Species
  • Quercetin