The world's first wiki where authorship really matters (Nature Genetics, 2008). Due credit and reputation for authors. Imagine a global collaborative knowledge base for original thoughts. Search thousands of articles and collaborate with scientists around the globe.

wikigene or wiki gene protein drug chemical gene disease author authorship tracking collaborative publishing evolutionary knowledge reputation system wiki2.0 global collaboration genes proteins drugs chemicals diseases compound
Hoffmann, R. A wiki for the life sciences where authorship matters. Nature Genetics (2008)
Chemical Compound Review

AC1LCT3P     4-[4-(4-aminophenoxy)phenyl]- 2-(4...

Synonyms: CTK0J6088, 228086-34-8
Welcome! If you are familiar with the subject of this article, you can contribute to this open access knowledge base by deleting incorrect information, restructuring or completely rewriting any text. Read more.

Disease relevance of Phthalazinone


High impact information on Phthalazinone

  • In the phthalazinone series, the cis-4a,5,6,7,8,8a-hexahydrophthalazinones and their corresponding 4a,5,8,8a-tetrahydro analogues showed potent PDE4 inhibitory potency (10/11c,d: pIC(50) = 7.6-8.4) [3].
  • Azelastine, a phthalazinone compound, is a second generation histamine H1 receptor antagonist which has shown clinical efficacy in relieving the symptoms of allergic rhinitis when administered as either an oral or intranasal formulation [4].
  • Azelastine, a phthalazinone derivative, is a new potent, long acting, orally active anti-allergic compound with particularly strong H1-histamine receptor antagonistic effects which has been proven to possess in vitro and in vivo a number of anti-inflammatory properties [5].
  • HP was metabolized by rat liver microsomes to products identified by HPLC and mass spectroscopy as s-triazolo[3,4-a]phthalazine (TP), 3-methyl-s-triazolo[3,4-a]phthalazine (MTP), phthalazine (P), and phthalazinone (PZ) [6].
  • 5 The ratios of the metabolites NAcHPZ/HH; TP/HH; NAcHPZ/PZ and PZ/TP are different in the two acetylator phenotypes [7].

Biological context of Phthalazinone

  • 6 It is possible the ratio PZ/TP may be used for determination of acetylator phenotype [7].
  • Several 5-substituted derivatives of 7-ethoxycarbonyl-6,8-dimethyl-1(2H)- phthalazinone were prepared by means of nitration, reductive amination, and diazonium decomposition [8].

Associations of Phthalazinone with other chemical compounds

  • P, PZ, and the unknown metabolite were established as oxidation products of HP using the model oxidative systems, metal-catalyzed autooxidation and horseradish peroxidase [6].

Gene context of Phthalazinone

  • We have previously described the discovery of poly(ADP-ribose)polymerase-1 (PARP-1) inhibitors based on a phthalazinone scaffold [9].

Analytical, diagnostic and therapeutic context of Phthalazinone


  1. Azamerone, a terpenoid phthalazinone from a marine-derived bacterium related to the genus streptomyces (actinomycetales). Cho, J.Y., Kwon, H.C., Williams, P.G., Jensen, P.R., Fenical, W. Org. Lett. (2006) [Pubmed]
  2. Effects of the phthalazinone azelastine on epidermal metabolism after mechanical skin irritation. Kietzmann, M., Lubach, D., Molliere, M., Szelenyi, I. Pharmacology (1992) [Pubmed]
  3. Novel selective PDE4 inhibitors. 1. Synthesis, structure-activity relationships, and molecular modeling of 4-(3,4-dimethoxyphenyl)-2H-phthalazin-1-ones and analogues. Van der Mey, M., Hatzelmann, A., Van der Laan, I.J., Sterk, G.J., Thibaut, U., Timmerman, H. J. Med. Chem. (2001) [Pubmed]
  4. Intranasal azelastine. A review of its efficacy in the management of allergic rhinitis. McNeely, W., Wiseman, L.R. Drugs (1998) [Pubmed]
  5. Effect of azelastine on the seasonal increase in non-specific bronchial responsiveness to methacholine in pollen allergic patients. A randomized, double-blind placebo-controlled, crossover study. Balzano, G., Gallo, C., Masi, C., Cocco, G., Ferranti, P., Melillo, E., Seccia, G. Clin. Exp. Allergy (1992) [Pubmed]
  6. The oxidative metabolism of hydralazine by rat liver microsomes. LaCagnin, L.B., Colby, H.D., O'Donnell, J.P. Drug Metab. Dispos. (1986) [Pubmed]
  7. Further evidence for an acetylator phenotype difference in the metabolism of hydralazine in man. Facchini, V., Timbrell, J.A. British journal of clinical pharmacology. (1981) [Pubmed]
  8. Studies on antiatherosclerotic agents. Synthesis of 5-substituted derivatives of 7-ethoxycarbonyl-6,8-dimethyl-1(2H) Eguchi, Y., Ishikawa, M. Chem. Pharm. Bull. (1991) [Pubmed]
  9. Phthalazinones 2: Optimisation and synthesis of novel potent inhibitors of poly(ADP-ribose)polymerase. Cockcroft, X.L., Dillon, K.J., Dixon, L., Drzewiecki, J., Kerrigan, F., Loh, V.M., Martin, N.M., Menear, K.A., Smith, G.C. Bioorg. Med. Chem. Lett. (2006) [Pubmed]
  10. Determination of hydralazine metabolites: 4-hydrazino-phthalazin-1-one and n-acetylhydrazinophthalazin-1-one by gas chromatography and s-triazolo[3,4-alpha]phthalazine and phthalazinone by high-performance liquid chromatography. Facchini, V., Timbrell, J.A. J. Chromatogr. (1980) [Pubmed]
WikiGenes - Universities