Phthalazin-1(2H)-one as a remarkable scaffold in drug discovery

Eur J Med Chem. 2015 Jun 5:97:462-82. doi: 10.1016/j.ejmech.2014.11.043. Epub 2014 Nov 25.

Abstract

Phthalazinones are an important kind of nitrogen atom containing heterocyclic compounds due to their synthetic and pharmacological versatility. This fused heterocycle system represents a common structural feature for many bioactive compounds showing a variety of pharmacological activities such as anticancer, anti-diabetic, anti-asthmatic, antihistaminic, antihypertensive, antithrombotic, anti-inflammatory, analgesic, antidepressant or antimicrobial agents, which makes it an attractive scaffold for the design and development of new drugs. This review summarizes detailed and updated information, described in recent non-patent literature, about the most relevant pharmacological properties of phthalazinone derivatives, highlighting the application of this potent pharmacophore in drug discovery.

Keywords: Azaheterocycle; Bioactive compound; Biological target; Pharmacological activity; Phthalazin-1(2H)-one; Synthesis.

Publication types

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

MeSH terms

  • Animals
  • Drug Design
  • Drug Discovery*
  • Heterocyclic Compounds / chemistry*
  • Heterocyclic Compounds / pharmacology*
  • Humans
  • Molecular Structure
  • Phthalazines / chemistry*
  • Phthalazines / pharmacology*
  • Structure-Activity Relationship

Substances

  • Heterocyclic Compounds
  • Phthalazines