Recent advance in oxazole-based medicinal chemistry

Eur J Med Chem. 2018 Jan 20:144:444-492. doi: 10.1016/j.ejmech.2017.12.044. Epub 2017 Dec 14.

Abstract

Oxazole compounds containing nitrogen and oxygen atoms in the five-membered aromatic ring are readily able to bind with a variety of enzymes and receptors in biological systems via diverse non-covalent interactions, and thus display versatile biological activities. The related researches in oxazole-based derivatives including oxazoles, isoxazoles, oxazolines, oxadiazoles, oxazolidones, benzoxazoles and so on, as medicinal drugs have been an extremely active topic, and numerous excellent achievements have been acquired. Noticeably, a large number of oxazole compounds as clinical drugs or candidates have been frequently employed for the treatment of various types of diseases, which have shown their large development value and wide potential as medicinal agents. This work systematically reviewed the recent researches and developments of the whole range of oxazole compounds as medicinal drugs, including antibacterial, antifungal, antiviral, antitubercular, anticancer, anti-inflammatory and analgesic, antidiabetic, antiparasitic, anti-obesitic, anti-neuropathic, antioxidative as well as other biological activities. The perspectives of the foreseeable future in the research and development of oxazole-based compounds as medicinal drugs are also presented. It is hoped that this review will serve as a stimulant for new thoughts in the quest for rational designs of more active and less toxic oxazole medicinal drugs.

Keywords: Biological activity; Medicinal chemistry; Oxazole.

Publication types

  • Review

MeSH terms

  • Analgesics / chemistry
  • Analgesics / pharmacology
  • Anti-Bacterial Agents / chemistry
  • Anti-Bacterial Agents / pharmacology
  • Anti-Inflammatory Agents, Non-Steroidal / chemistry
  • Anti-Inflammatory Agents, Non-Steroidal / pharmacology
  • Anti-Obesity Agents / chemistry
  • Anti-Obesity Agents / pharmacology
  • Antifungal Agents / chemistry
  • Antifungal Agents / pharmacology
  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / pharmacology
  • Antioxidants / chemistry
  • Antioxidants / pharmacology
  • Antiparasitic Agents / chemistry
  • Antiparasitic Agents / pharmacology
  • Antitubercular Agents / chemistry
  • Antitubercular Agents / pharmacology
  • Antiviral Agents / chemistry
  • Antiviral Agents / pharmacology
  • Chemistry, Pharmaceutical
  • Humans
  • Hypoglycemic Agents / chemistry
  • Hypoglycemic Agents / pharmacology
  • Molecular Structure
  • Oxazoles / chemistry
  • Oxazoles / pharmacology*

Substances

  • Analgesics
  • Anti-Bacterial Agents
  • Anti-Inflammatory Agents, Non-Steroidal
  • Anti-Obesity Agents
  • Antifungal Agents
  • Antineoplastic Agents
  • Antioxidants
  • Antiparasitic Agents
  • Antitubercular Agents
  • Antiviral Agents
  • Hypoglycemic Agents
  • Oxazoles