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Novel antiasthmatic agents with dual activities of thromboxane A2 synthetase inhibition and bronchodilation. 1. 2-[2-(1-imidazolyl)alkyl]- 1(2H)-phthalazinones

A number of 4-substituted 2-[omega-(1-imidazolyl)alkyl]-1(2H)-phthalazinones were synthesized in order to develop agents possessing both thromboxane A2 synthetase inhibitory and bronchodilatory activities. The pharmacological evaluation of these compounds disclosed that they have both activities to various extents. Both activities were slightly dependent on the length of the 2-substituents and largely affected by the nature of the 4-substituents. Compounds bearing phenyl and thienyl groups exhibited relatively high and well-rounded activities. Among these compounds, 12j and 15f were found to be the most effective agents having well-rounded activities in vitro and in vivo. Introduction of a carboxyl group reduced both activities contrary to our expectation. 4-(3-Pyridyl)phthalazinone 18b was of particular interest because of unexpectedly high in vivo activities in spite of an absence of significant in vitro activities.

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Phthalazine – Wikipedia,
Phthalazine | C8H6N732 – PubChem

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Ring-rearrangement during the Mitsunobu alkylation of phthalazinones and indazolols

The Mitsunobu alkylation of substituted phthalazinones and indazolols with cyclic hydroxy- and hydroxymethyl-substituted amines was investigated. In addition to the expected derivatives ring-narrowed and ring-enlarged rearrangement products were isolated and characterized by NMR spectroscopy. The occurence of these products can be explained by the existence of a bicyclic intermediate. The results of the reaction of phthalazinones with optically active amine compounds show a stereospecific reaction mechanism. The reaction of the phthalazinones leads to N-substituted products, while in the case of the indazolols O-substituted derivatives were isolated. A postulated bicyclic intermediate, 1-methyl-1-azoniabicyclo[3.2.0]heptane, was synthesized as chloride. VCH Verlagsgesellschaft mbH, 1996.

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Phthalazine – Wikipedia,
Phthalazine | C8H6N727 – PubChem

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PHENYL PHTHALAZINE DERIVATIVE, METHOD FOR THE PREPARATION THEREOF, AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME

The present invention relates to a compound represented by Chemical Formula 1, or a pharmaceutically acceptable salt thereof. The compound according to the present invention can be usefully used for the prevention or treatment of cardiovascular diseases.

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Phthalazine – Wikipedia,
Phthalazine | C8H6N720 – PubChem

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Vasorelaxant activity of phthalazinones and related compounds

Several series of dihydrostilbenamide, imidazo[2,1-a]isoindole, pyrimido[2,1-a]isoindole and phthalazinone derivatives were obtained and their vasorelaxant activity was measured on isolated rat aorta rings pre-contracted with phenylephrine (10-5 M). Some phthalazinones attained, practically, the total relaxation of the organ at micromolar concentrations. For the most potent compound 9h (EC50 = 0.43 muM) the affinities for alpha1A, alpha1B and alpha1D adrenergic sub-receptors were determined.

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Phthalazine – Wikipedia,
Phthalazine | C8H6N730 – PubChem

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The discovery of phthalazinone-based human H1 and H3 single-ligand antagonists suitable for intranasal administration for the treatment of allergic rhinitis

A series of potent phthalazinone-based human H1 and H 3 bivalent histamine receptor antagonists, suitable for intranasal administration for the potential treatment of allergic rhinitis, were identified. Blockade of H3 receptors is thought to improve efficacy on nasal congestion, a symptom of allergic rhinitis that is currently not treated by current antihistamines. Two analogues (56a and 56b) had slightly lower H1 potency (pA2 9.1 and 8.9, respectively, vs 9.7 for the clinical gold-standard azelastine, and H3 potency (pK i 9.6 and 9.5, respectively, vs 6.8 for azelastine). Compound 56a had longer duration of action than azelastine, low brain penetration, and low oral bioavailability, which coupled with the predicted low clinical dose, should limit the potential of engaging CNS-related side-effects associated with H 1 or H3 antagonism.

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Phthalazine – Wikipedia,
Phthalazine | C8H6N731 – PubChem

One of the major reasons for studying chemical kinetics is to use measurements of the macroscopic properties of a system, Quality Control of 4-(4-Chlorobenzyl)phthalazin-1(2H)-one, such as the rate of change in the concentration of reactants or products with time.In a article, mentioned the application of 53242-88-9, Name is 4-(4-Chlorobenzyl)phthalazin-1(2H)-one, molecular formula is C15H11ClN2O

Synthesis, bioevaluation and structural study of substituted phthalazin-1(2H)-ones acting as antifungal agents

Twenty-five polysubstituted phthalazinone derivatives were synthesized and tested for their antifungal activity against a panel of pathogenic and clinically important yeasts and filamentous fungi. Among them, the compound 4-(4-chlorobenzyl)-2- methylphthalazin-1(2H)-one (5) exhibited a remarkable antifungal activity against standardised strains of dermatophytes and Cryptococcus neoformans, as well as against some clinical isolates. A physicochemical study performed on compound 5 revealed its conformational and electronic characteristics, providing us with useful data for the future design of novel related antifungal analogues.

Sometimes chemists are able to propose two or more mechanisms that are consistent with the available data. Quality Control of 4-(4-Chlorobenzyl)phthalazin-1(2H)-one, If a proposed mechanism predicts the wrong experimental rate law, however, the mechanism must be incorrect.Welcome to check out more blogs about 53242-88-9, in my other articles.

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Phthalazine – Wikipedia,
Phthalazine | C8H6N724 – PubChem

In homogeneous catalysis, the catalyst is in the same phase as the reactant. The number of collisions between reactants and catalyst is at a maximum.In a patent, 53242-88-9, name is 4-(4-Chlorobenzyl)phthalazin-1(2H)-one, introducing its new discovery. COA of Formula: C15H11ClN2O

Aminocarboxylic acid derivatives having antiallergic/antiasthmatic effect and a process for their preparation

6-amino carboxylic acid derivatives having antiasthmatic and antiallergic properties which can be used for the preparation of medicaments. The compounds have the formula: STR1 wherein R1 and R2 represent hydrogen, a straight-chain or branched alkyl radical with 1-6 carbon atoms, benzyl or phenylethyl, R3 represents hydrogen, a straight-chain or branched alkyl radical with 1-6 carbon atoms or benzyl, X represents hydrogen, halogen, C1 -C6 -alkyl or C1 -C6 -alkoxy, Y1 and Y2 represent hydrogen, halogen, C1 -C6 -alkyl or C1 -C6 -alkoxy, where m, n and o can assume the values from 0-4.

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Phthalazine – Wikipedia,
Phthalazine | C8H6N717 – PubChem

One of the major reasons for studying chemical kinetics is to use measurements of the macroscopic properties of a system, SDS of cas: 53242-88-9, such as the rate of change in the concentration of reactants or products with time.In a article, mentioned the application of 53242-88-9, Name is 4-(4-Chlorobenzyl)phthalazin-1(2H)-one, molecular formula is C15H11ClN2O

Anti-HIV activity of stilbene-related heterocyclic compounds

Viral transcription has not been routinely targeted in the development of new antiviral drugs. This crucial step of the viral cycle depends on the concerted action of cellular and viral proteins such as NF-kappaB and Tat. In the present study, stilbene-related heterocyclic compounds including benzalphthalide, phthalazinone, imidazoindole and pyrimidoisoindole derivatives are tested for their anti-HIV activity. Original assays based on recombinant viruses were used to evaluate HIV replication inhibition and stably transfected cell lines were used to evaluate inhibition of Tat and NF-kappaB proteins. Some of the stilbene-related heterocyclic compounds analysed displayed anti-HIV activity through interference with NF-kappaB and Tat function. Moreover, compounds inhibiting both targets displayed a stronger activity on viral replication.

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Phthalazine – Wikipedia,
Phthalazine | C8H6N721 – PubChem

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The imidazo[2,1-a]isoindole system. A new skeletal basis for antiplasmodial compounds

The in vitro antiplasmodial activity of some dihydrostilbenamides, phtalazinones, imidazo[2,1-a]isoindole and pyrimido[2,1-a]isoindole derivatives related to the natural dihydrostilbenoid isonotholaenic acid is reported. The evaluation was performed on cultures of F32 strain of Plasmodium falciparum and potent representative compounds were also evaluated in the ferriprotoporphyrin IX biomineralization inhibition test (FBIT). Compounds having the imidazo[2,1-a]isoindole skeleton were the most active and one compound of this group resulted to be as potent as chloroquine, but acting through a mechanism different that of the inhibition of heme biomineralization.

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Phthalazine – Wikipedia,
Phthalazine | C8H6N723 – PubChem

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Leishmanicidal activity of some stilbenoids and related heterocyclic compounds

We have evaluated the leishmanicidal activity of some natural and semisynthetic dihydrostilbenoids and several compounds of other series of dihydrostilbamides, isoindoles, phthalazinones, imidazoisoindoles and pyrimidoisoindoles. The evaluation was performed in vitro, on cultures of cutaneous, mucocutaneous and visceral strains of Leishmania spp. The most potent and selective compounds of these series were the dihydrostilbene piperidides.

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Phthalazine – Wikipedia,
Phthalazine | C8H6N722 – PubChem