New explortion of 4,5-Dichloro-3(2H)-pyridazinone

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IMIDAZOLES

The present invention relates to imidazole derivatives of the general formulawherein R1, R2, R3, and R4 are as defined in the specification and to pharmaceutically acceptable salts thereof. Compounds of formula I are metabotropic glutamate receptor antagonists. They can be used in the treatment or prevention of mGluR5 receptor mediated disorders.

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Pyridazine | C4H4N2250 – PubChem

 

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Studies on improved synthesis of 2?-deoxyribonucleosides of pyridazine derivatives

A number of 2?-deoxyribonucleosides of halogenated pyridazine derivatives were prepared by glycosylation of their respective potassium or DBU salts in acetone. The reaction yielded predominatly beta-anomers that could be purified by simple crystallization or column chromatography. Of the studied pyridazines and deoxynucleosides, only 4-bromo-6-chloro-pyridazin-3-one and 6-chloro-2-(2?-deoxyribofuranosyl)pyridazin-3-one showed modest inhibition of CK2 kinase.

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Can You Really Do Chemisty Experiments About 3-Phenyl-6-chloropyridazine

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ALKYL-SUBSTITUTED 3′ COMPOUNDS HAVING 5-HT6 RECEPTOR AFFINITY

The present disclosure provides compounds having affinity for the 5-HT6 receptor which are of the formula (I): wherein R1, R2, Ar, m and n are as defined herein. The disclosure also relates to methods of preparing such compounds, compositions containing such compounds, and methods of use thereof.

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Pyridazine | C4H4N2559 – PubChem

 

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Synthesis of Some Imidazole- and Pyrazole- Derived Chelating Agents

Procedures involving condensation of o-phenylenediamines with carboxylic acids, and reaction of bifunctional alkyl halides with bifunctional nucleophiles are described.Syntheses are reported of 2,6-bis(2-benzimidazyl)-pyridine, 1,3-bis(2-benzimidazyl)-2-thiapropane, 1,7-bis(2-benzimidazyl)-2,6-dithiaheptane, 2-hydroxymethyl-5,6-dimethylbenzimidazole, 2-chloromethyl-5,6-dimethylbenzimidazole hydrochloride, 1,7-bis(5,6-dimethyl-2-benzimidazyl)-2,6-dithiaheptane, 3,6-bis(1-pyrazolyl)pyridazine, 2-(2-hydroxy-3-methylphenyl)benzimidazole, 2-(2-hydroxyphenyl)benzimidazole, 5-(2-hydroxyphenyl)-3-methyl-1-phenylpyrazole, 3(5)-(2-hydroxyphenyl)-5(3)-methylpyrazole, 3(5)-(2-hydroxyphenyl)-5(3)-phenylpyrazole, and 1,3-bis((5-methylpyridyl)imino)isoindoline.

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Final Thoughts on Chemistry for 3-Piperazin-1-yl-pyridazine

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New arylpiperazine derivatives as antagonists of the human cloned 5-HT4 receptor isoforms

New derivatives of arylpiperazine 9 were designed from ML 10302, a potent 5-HT4 receptor agonist in the gastrointestinal system. Compounds were synthesized by condensation of a number of available arylpiperazines or heteroarylpiperazines with 2-bromoethyl 4-amino-5-chloro-2-methoxybenzoate. They were evaluated in binding assays on the recently cloned human 5-HT(4(e)) isoform stably expressed in C6 glial cells with [3H]GR 113808 as the radioligand. The affinity values (K(i)) depended upon the substituent on the aromatic ring. A chlorine atom produced a marked drop in activity (K(i) > 100 nM), while a m-methoxy group gave a compound with nanomolar affinity (K(i) = 3 nM). The most potent compounds were the heterocyclic derivatives with pyrimidine, pyrazine, pyridazine, or pyridine moieties (compounds 9r, 9t, 9u, 9x, respectively). K(i) values for 9a and 9r were determined for the 5-HT(4(a)), 5-HT(4(b)), 5-HT(4(c)), and 5-HT(4(d)) receptor isoforms transiently expressed in COS cells. The results indicated that the compounds were not selective. They produced an inhibition of the 5-HT-stimulated cyclic AMP synthesis in the C6 glial cells stably expressing the 5-HT(4(e)) receptor and shifted the 5-HT concentration-effect curve on adenylyl cyclase activity with pK(D) values of 7.44 and 8.47, respectively. In isolated human atrial myocytes, 9r antagonized the stimulatory effect of 5-HT on the L-type calcium current (I(Ca)) with a K(D) value of 0.7 nM.

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Retro-ene reactions. III. Alkylation of 4,5-dichloro-1-hydroxymethylpyridazin-6-ones: Synthesis of 4,5-dichloro-1-(omega-phthalimido and saccharin-2?-ylalkyl)pyridazin-6-ones

4,5-Dichloro-1-(omega-phthalimido and saccharinyl-2?-ylalkyl)pyridazin-6-ones were synthesized from 4,5-dichloro-1-hydroxymethylpyridazin-6-one and the corresponding N-(omega-haloalkyl)phthalimides and saccharins via a fragmentation of retro-ene type.

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New explortion of 3-Chloro-6-methylpyridazine

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Room-Temperature Arylation of Thiols: Breakthrough with Aryl Chlorides

The formation of aryl C?S bonds is an important chemical transformation because aryl sulfides are valuable building blocks for the synthesis of biologically and pharmaceutically active molecules and organic materials. Aryl sulfides have traditionally been synthesized through the transition-metal-catalyzed cross-coupling of aryl halides with thiols. However, the aryl halides used are usually bromides and iodides; readily available, low-cost aryl chlorides often not reactive enough. Furthermore, the deactivation of transition-metal catalysts by thiols has forced chemists to use high catalyst loadings, specially designed ligands, high temperatures, and/or strong bases, thus leading to high costs and the incompatibility of some functional groups. Herein, we describe a simple and efficient visible-light photoredox arylation of thiols with aryl halides at room temperature. More importantly, various aryl chlorides are also effective arylation reagents under the present conditions.

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Properties and Exciting Facts About 3,6-Dichloropyridazine

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Selective fluorination by halogen exchange of chlorodiazines and chloropyridines promoted by the ‘proton sponge’ – Triethylamine tris(hydrogen fluoride) system

The ‘proton sponge’ – triethylamine tris(hydrogen fluoride) mixtures provide a mild and efficient fluorinating reagent to introduce selectively fluorine atoms by halogen exchange into chlorodiazines and chloronitropyridine series.

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Simple exploration of 2164-61-6

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Design, synthesis and antibacterial properties of pyrimido[4,5-b]indol-8-amine inhibitors of DNA gyrase

According to the World Health Organization (WHO), approximately 1.7 million deaths per year are caused by tuberculosis infections. Furthermore, it has been predicted that, by 2050, antibacterial resistance will be the cause of approximately 10 million deaths annually if the issue is not tackled. As a result, novel approaches to treating broad-spectrum bacterial infections are of vital importance. During the course of our wider efforts to discover unique methods of targeting multidrug-resistant (MDR) pathogens, we identified a novel series of amide-linked pyrimido[4,5-b]indol-8-amine inhibitors of bacterial type II topoisomerases. Compounds from the series were highly potent against gram-positive bacteria and mycobacteria, with excellent potency being retained against a panel of relevant Mycobacterium tuberculosis drug-resistant clinical isolates.

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Some scientific research about 3-Chloro-6-methylpyridazine

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Antipicornaviral pyridazinamines

Piperidinyl, pyrrolidinyl, azepinyl and piperazinyl pyridazines of formula STR1 wherein one or two carbon atoms of the STR2 moiety may be substituted with C1-4 alkyl, C1-4 alkyloxy or two carbon atoms of the CH2 groups of said moiety may be bridged with a C2-4 alkanediyl radical; X represents CH or N; R1 represents hydrogen, C1-4 alkyl, halo, hydroxy, trifluoromethyl, cyano, C1-4 alkyloxy, C1-4 alkylthio, C1-4 alkylsulfinyl, C1-4 alkylsulfonyl, C1-4 alkyloxycarbonyl, C1-4 alkylcarbonyl or aryl; R2 and R3 each independently represent hydrogen or C1-4 alkyl; Alk represents C1-4 alkanediyl; R4 and R5 each independently represent hydrogen, C1-4 alkyl or halo; and Het represents STR3 the addition salts and stereochemically isomeric forms thereof, said compounds having antipicornaviral activity. Pharmaceutical compositions containing these compounds as active ingredient, and a method of preparing said compounds and pharmaceutical compositions.

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