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Chemical Compound Review:

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

Synonyms: CTK0J6088, 228086-34-8

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Disease relevance of Phthalazinone

Azamerone, a terpenoid phthalazinone from a marine-derived bacterium related to the genus streptomyces (actinomycetales) [1].
Therefore, a beneficial role of this phthalazinone in the treatment of psoriasis and related skin disorders seems to be possible [2].

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

Phthalazinone and s-triazolo[3,4-alpha]phthalazine are measured underivatised by high-performance liquid chromatography [10].

References

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]
Effects of the phthalazinone azelastine on epidermal metabolism after mechanical skin irritation. Kietzmann, M., Lubach, D., Molliere, M., Szelenyi, I. Pharmacology (1992) [Pubmed]
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]
Intranasal azelastine. A review of its efficacy in the management of allergic rhinitis. McNeely, W., Wiseman, L.R. Drugs (1998) [Pubmed]
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]
The oxidative metabolism of hydralazine by rat liver microsomes. LaCagnin, L.B., Colby, H.D., O'Donnell, J.P. Drug Metab. Dispos. (1986) [Pubmed]
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]
Studies on antiatherosclerotic agents. Synthesis of 5-substituted derivatives of 7-ethoxycarbonyl-6,8-dimethyl-1(2H)-phthalazinone.off. Eguchi, Y., Ishikawa, M. Chem. Pharm. Bull. (1991) [Pubmed]
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]
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]

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