title: Phthalazin-1(2H)-one as a remarkable scaffold in drug discovery.
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.
authors.affiliation: Departamento de Química Orgánica and Instituto de Investigación Biomédica (IBI), Universidade de Vigo, 36310 Vigo, Spain.
authors.forename: Noemí
authors.initials: N
authors.lastname: Vila
authors.affiliation: Departamento de Química Orgánica and Instituto de Investigación Biomédica (IBI), Universidade de Vigo, 36310 Vigo, Spain.
authors.forename: Pedro
authors.initials: P
authors.lastname: Besada
authors.affiliation: Departamento de Química Orgánica and Instituto de Investigación Biomédica (IBI), Universidade de Vigo, 36310 Vigo, Spain.
authors.forename: Tamara
authors.initials: T
authors.lastname: Costas
authors.affiliation: Departamento de Química Orgánica and Instituto de Investigación Biomédica (IBI), Universidade de Vigo, 36310 Vigo, Spain.
authors.forename: M Carmen
authors.initials: MC
authors.lastname: Costas-Lago
authors.affiliation: Departamento de Química Orgánica and Instituto de Investigación Biomédica (IBI), Universidade de Vigo, 36310 Vigo, Spain. Electronic address: mcteran@uvigo.es.
authors.forename: Carmen
authors.initials: C
authors.lastname: Terán
mesh_terms: D000818:Animals; D015195:Drug Design; D055808:Drug Discovery; D006571:Heterocyclic Compounds / Q000737:chemistry* / Q000494:pharmacology*; D006801:Humans; D015394:Molecular Structure; D010793:Phthalazines / Q000737:chemistry* / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D006571:Heterocyclic Compounds; D010793:Phthalazines
keywords: Azaheterocycle; Bioactive compound; Biological target; Pharmacological activity; Phthalazin-1(2H)-one; Synthesis