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Seasonal and pandemic influenza outbreaks remain a major human health problem. Inhibition of the endonuclease activity of influenza RNA-dependent RNA polymerase is attractive for the development of new agents for the treatment of influenza infection. Our earlier studies identified a series of 5- and 6-phenyl substituted 3-hydroxypyridin-2(1H)-ones that were effective inhibitors of influenza endonuclease. These agents identified as bimetal chelating ligands binding to the active site of the enzyme. In the present study, several aza analogues of these phenyl substituted 3-hydroxypyridin-2(1H)-one compounds were synthesized and evaluated for their ability to inhibit the endonuclease activity. In contrast to the 4-aza analogue of 6-(4-fluorophenyl)-3-hydroxypyridin-2(1H)-one, the 5-aza analogue (5-hydroxy-2-(4-fluorophenyl)pyrimidin-4(3H)-one) did exhibit significant activity as an endonuclease inhibitor. The 6-aza analogue of 5-(4-fluorophenyl)-3-hydroxypyridin-2(1H)-one (6-(4-fluorophenyl)-4-hydroxypyridazin-3(2H)-one) also retained modest activity as an inhibitor. Several varied 6-phenyl-4-hydroxypyridazin-3(2H)-ones and 2-phenyl-5-hydroxypyrimidin-4(3H)-ones were synthesized and evaluated as endonuclease inhibitors. The SAR observed for these aza analogues are consistent with those previously observed with various phenyl substituted 3-hydroxypyridin-2(1H)-ones.

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Reference:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2355 – PubChem

 

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Some pyridazine acyclonucleosides containing hydroxymethyl and 4-hydroxybutyl groups as an alkanol side chain were prepared. Nucleophilic displacement of N1-alkyl-4,5-dichloropyridazin-6-ones is discussed.

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Pyridazine – Wikipedia,
Pyridazine | C4H4N2307 – PubChem

 

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The synthesis of a series of 5-(4-piperazinyl)-3(2H)-pyridazinone has been reported. The blocking activity of these compounds was determined on the pre- and postsynaptic alpha-adrenoreceptors of isolated rat vas deferens.

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Reference:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2312 – PubChem

 

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(6-Oxo-6H-pyridazin-1-yl)phosphoric acid diethyl esters (3) are efficient and selective coupling agents for equimolar esterification of carboxylic acids and alcohols. Esterification of aliphatic and aromatic carboxylic acids with aliphatic and aromatic alcohols using 3 afforded the corresponding esters chemoselectively in good to excellent yield.

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Reference:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2374 – PubChem

 

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The novel 7-transmembrane receptor MrgX1 is located predominantly in the dorsal root ganglion and has consequently been implicated in the perception of pain. Here we describe the discovery and optimization of a small molecule agonist and initial docking studies of this ligand into the receptor in order to provide a suitable lead and tool compound for the elucidation of the physiological function of the receptor.

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Reference:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2376 – PubChem

 

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4-Substitued azaindolines, which are isosteres of indolines, are useful synthetic building blocks that reduce the risk of bioactivation induced idiosyncratic toxicity have been prepared. Multigram routes to 2,3-dihydro-1H-pyrrolo[2,3-c]pyridine-4-triflate 16, 2,3-dihydro-1H-pyrrolo[2,3- b]pyridine-4-carbonitrile 20 and 4-chloro-2,3-dihydro-1H-pyrrolo[2,3-d] pyridazine 30 are outlined.

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Reference:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2352 – PubChem

 

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Aiming to discover melanin-concentrating hormone receptor 1 (MCHR1) antagonists with improved safety profiles, we hypothesized that the aliphatic amine employed in most antagonists reported to date could be removed if the bicyclic motif of the compound scaffold interacted with Asp123 and/or Tyr272 of MCHR1. We excluded aliphatic amines from our compound designs, with a cutoff value of pKa < 8, and explored aliphatic amine-free MCHR1 antagonists in a CNS-oriented chemical space limited by four descriptors (TPSA, ClogP, MW, and HBD count). Screening of novel bicyclic motifs with high intrinsic binding affinity for MCHR1 identified the imidazo[1,2-a]pyridine ring (represented in compounds 6a and 6b), and subsequent cyclization of the central aliphatic amide linkage led to the discovery of a potent, orally bioavailable MCHR1 antagonist 4-[(4-chlorobenzyl)oxy]-1-(2-cyclopropyl-3-methylimidazo[1,2-a]pyridin-6-yl)pyridin-2(1H)-one 10a. It exhibited low potential for hERG inhibition and phospholipidosis induction as well as sufficient brain concentration to exert antiobesity effects in diet-induced obese rats. If you are interested in 932-22-9, you can contact me at any time and look forward to more communication. Computed Properties of C4H2Cl2N2O

Reference:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2320 – PubChem

 

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932-22-9, Name is 4,5-Dichloro-3(2H)-pyridazinone, belongs to pyridazine compound, is a common compound. Application In Synthesis of 4,5-Dichloro-3(2H)-pyridazinoneIn an article, once mentioned the new application about 932-22-9.

1-Alkyl-4,5-dichloropyridazin-6-ones and (4,5-dichloro-6-oxopyridazin-1-yl)methylcarboxylates were synthesized from 4,5-dichloro-1-hydroxymethylpyridazin-6-one and the corresponding alkyl halides or carboxylic acid chlorides. Also the reaction mechanisms via a fragmentation of retro-ene type are discussed.

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Reference:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2332 – PubChem

 

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One of the major reasons for studying chemical kinetics is to use measurements of the macroscopic properties of a system, Quality Control of 4,5-Dichloro-3(2H)-pyridazinone, such as the rate of change in the concentration of reactants or products with time.In a article, mentioned the application of 932-22-9, Name is 4,5-Dichloro-3(2H)-pyridazinone, molecular formula is C4H2Cl2N2O

A series of new pyridazin-3(2H)-one derivatives (3 and 4) were evaluated for their in vitro affinity toward both alpha1- and alpha2-adrenoceptors by radioligand receptor binding assays. All target compounds showed good affinities for the alpha1-adrenoceptor, with Ki values in the low nanomolar range. The polymethylene chain constituting the spacer between the furoylpiperazinyl pyridazinone and the arylpiperazine moiety was shown to influence the affinity and selectivity of these compounds. Particularly, a gradual increase in affinity was observed by lengthening the polymethylene chain up to a maximum of seven carbon atoms. In addition, compound 3k, characterized by a very interesting alpha1-AR affinity (1.9 nM), was also shown to be a highly selective alpha1-AR antagonist, the affinity ratio for alpha2- and alpha1-adrenoceptors being 274. To gain insight into the structural features required for alpha1 antagonist activity, the pyridazinone derivatives were submitted to a pharmacophore generation procedure using the program Catalyst. The resulting pharmacophore model showed high correlation and predictive power. It also rationalized the relationships between structural properties and biological data of, and external to, the pyridazinone class.

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Reference:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2292 – PubChem

 

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The invention relates to a oxadiazole compound and its preparation method, the compound of the formula as follows: wherein R1is halogen, hydrogen, 1 – 4 carbon atoms or alkoxy, R2is halogen, hydrogen or alkyl, R3is methylamine, dimethylamine, isopropylamine, propylamine, butylamine, morpholine, piperidine or imidazole. Compared with the prior art, the process of the invention the procedure is simple, wide application range, suitable for use in the health pests such as flies, mosquitoes, flea and a drop shape and agricultural pests aqueous phase armor, Spodoptera exigua, insects and other pests on, can inhibit the growth of the mosquitoes for insect in particular, is a kind of have application prospect of insecticide. (by machine translation)

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Reference:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2255 – PubChem