Month: November 2022

Gokce, Mehtap published the artcileSynthesis and antinociceptive activity of 6-substituted 3-pyridazinone derivatives, Formula: C8H10ClN3O, the main research area is pyridazinone morpholino arylpiperidino arylpiperazino preparation antinociceptive activity; antinociceptive activity morpholinopyridazinone arylpiperidinopyridazinone arylpiperazinopyridazinone.

Title compounds I (X = O, CH-benzyl, N-benzyl, N-aryl) were prepared and evaluated for antinociceptive activity. In the modified Koster test in mice, I (X = NC6H4F-4) was the most active compound All the compounds except I (X = NPh) were more active than aspirin in the antinociceptive activity test.

Farmaco published new progress about Analgesics. 17259-32-4 belongs to class pyridazine, name is 4-(6-Chloropyridazin-3-yl)morpholine, and the molecular formula is C8H10ClN3O, Formula: C8H10ClN3O.

Referemce:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem

Landquist, Justus K. published the artcilePyridazines. II. Reaction of polychloropyridazines with trimethylamine, Category: pyridazine, the main research area is chloropyridazine amination; pyridazines chloro amination; triazine chloro amination; pyrimidines chloro amination; cyanuric chloride amination; trimethylamine amination pyridazines; ammoniums pyridazines.

3,6-Dichloro-, 3,4,6-trichloro-, 3,4,5-trichloro-, and 3,4,5,6-tetrachloropyridazine reacted with Me3N to give trimethylpyridazinylammonium chlorides, which, with the exception of (5,6-dichloro-3-pyridazinyl)ammonium chloride, underwent demethylation in the reaction mixture at room temperature to give (dimethylamino)pyridazines. The position of substitution was governed by steric requirements. 4,6-Dichloropyrimidine, 4,5,6-trichloropyrimidine, cyanuric chloride, and 4-butoxy-3,6-dichloropyridazine were also dimethylaminated by Me3N.

Journal of the Chemical Society [Section] C: Organic published new progress about Demethylation. 7145-60-0 belongs to class pyridazine, name is 6-Chloro-N,N-dimethylpyridazin-3-amine, and the molecular formula is C6H8ClN3, Category: pyridazine.

Referemce:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem

Alagoz, Mehmet Abdullah published the artcileDevelopment of a Novel Class of Pyridazinone Derivatives as Selective MAO-B Inhibitors, HPLC of Formula: 17259-32-4, the main research area is pyridazinone derivative development MAOB inhibitor; PAMPA; docking; kinetics; monoamine oxidase-B; pyridazinones; reversibility.

Sixteen compounds (TR1-TR16) were synthesized and evaluated for their inhibitory activities against monoamine oxidase A and B (MAOs). Most of the derivatives showed potent and highly selective MAO-B inhibition. Compound TR16 was the most potent inhibitor against MAO-B with an IC50 value of 0.17 μM, followed by TR2 (IC50 = 0.27 μM). TR2 and TR16 selectivity index (SI) values for MAO-B vs. MAO-A were 84.96 and higher than 235.29, resp. Compared to the basic structures, the para-chloro substituent in TR2 and TR16 increased the inhibitory activity of MAO-B. TR2 and TR16 were reversible MAO-B inhibitors that were competitive, with Ki values of 0.230 ± 0.004 and 0.149 ± 0.016 μM, resp. The PAMPA method indicated that compounds TR2 and TR16 had the tendency to traverse the blood-brain barrier. Docking investigations revealed that lead compounds were beneficial for MAO-B inhibition via association with key as well as selective E84 or Y326 residues, but not for MAO-A inhibition via interaction primarily driven by hydrophobic contacts. In conclusion, TR2 and TR16 are therapeutic prospects for the management of multiple neurodegenerative diseases.

Molecules published new progress about Bioavailability. 17259-32-4 belongs to class pyridazine, name is 4-(6-Chloropyridazin-3-yl)morpholine, and the molecular formula is C8H10ClN3O, HPLC of Formula: 17259-32-4.

Referemce:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem

Hallot, Andre published the artcileSynthesis and activity of 6-aryl-3-(hydroxypolymethyleneamino)pyridazines in animal models of epilepsy, Quality Control of 58059-33-9, the main research area is hydroxypolymethyleneamino pyridazine preparation anticonvulsant; piperidinopyridazine chlorophenylhydroxy preparation anticonvulsant.

Title pyridazines, e.g. I (R = ClC6H4, Cl2C6H3, thienyl, pyridyl), were synthesized and evaluated for anticonvulsant activity. The compounds were screened in mice for their ability to antagonize maximal electroshock- and bicuculline-induced seizures; neurotoxicity was evaluated in the rotorod test. The anticonvulsant activity of the most potent compounds was examined in kindled amygdaloid rats and in photoepileptic Papio papio baboons. Structure-activity relationships were examined by either varying the aryl ring in the 6-position of the pyridazine ring or by modifying the 3-amino side chain. Only the compounds with a Ph ring in the 6-position of the pyridazine ring exhibited appreciable anticonvulsant activity, and a 4-hydroxypiperidine side chain in the 3-position of the pyridazine ring appeared essential for anticonvulsant activity. Substituting the Ph ring with a Cl in the 2-position led to a substantial increase of activity and disubstituting the Ph ring with a Cl in the 2- and 4-positions yielded the most potent compounds, some of which were as potent as, or more potent than, phenobarbital. 6-(2-Chlorophenyl)-3-(4-hydroxypiperidino)pyridazine and 6-(2,4-dichlorophenyl-3-(4-hydroxypiperidino)pyridazine were selected for further studies.

Journal of Medicinal Chemistry published new progress about Anticonvulsants. 58059-33-9 belongs to class pyridazine, name is 3-Chloro-6-(3-nitrophenyl)pyridazine, and the molecular formula is C10H6ClN3O2, Quality Control of 58059-33-9.

Referemce:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem

Sengmany, Stephane published the artcileSynthesis and biological evaluation of 3-amino-, 3-alkoxy- and 3-aryloxy-6-(hetero)arylpyridazines as potent antitumor agents, Formula: C6H8ClN3, the main research area is aryl pyridazine preparation antitumor toxicity human; chloropyridazine aryl halide electrochem reductive coupling nickel catalyst; Arylpyridazines; Biological evaluation; Cytotoxic activity; Electrosynthesis; Nickel catalysis.

Various 3-amino-6-arylpyridazines I [R = Me2N, pyrrol-1-yl, morpholino, etc.; Ar = C6H5, 3-MeC6H4, 3-thienyl, etc.] and 3-aryloxy- and alkoxy-6-arylpyridazines II [R1 = Et, C6H5, 4-FC6H4, etc.] were synthesized by an electrochem. reductive cross-coupling between chloropyridazines and aryl or heteroaryl halides. In vitro antiproliferative activity of these products I and II was evaluated against a representative panel of cancer cell lines and oncogenicity prevention of the more efficient derivatives was highlighted on human breast cancer cell line MDA-MB 468-Luc prior establishing their interaction with p44/42 and Akt-dependent signaling pathways. The highest in vitro antiproliferative activity was found for compound I [R = Et2N; Ar = 4-MeO2CC6H4] and also showed a potent ability to inhibit clonogenicity of human breast cancer cell line. The toxicity of the most active compounds I [R = Et2N; Ar = 4-MeO2CC6H4, 4-EtO2CC6H4] was further evaluated in vitro on human hepatocytes and in vivo on zebrafish assays.

Bioorganic & Medicinal Chemistry Letters published new progress about Antitumor agents. 7145-60-0 belongs to class pyridazine, name is 6-Chloro-N,N-dimethylpyridazin-3-amine, and the molecular formula is C6H8ClN3, Formula: C6H8ClN3.

Referemce:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem

Sengmany, Stephane published the artcileSynthesis and biological evaluation of 3-amino-, 3-alkoxy- and 3-aryloxy-6-(hetero)arylpyridazines as potent antitumor agents, Safety of 4-(6-Chloropyridazin-3-yl)morpholine, the main research area is aryl pyridazine preparation antitumor toxicity human; chloropyridazine aryl halide electrochem reductive coupling nickel catalyst; Arylpyridazines; Biological evaluation; Cytotoxic activity; Electrosynthesis; Nickel catalysis.

Various 3-amino-6-arylpyridazines I [R = Me2N, pyrrol-1-yl, morpholino, etc.; Ar = C6H5, 3-MeC6H4, 3-thienyl, etc.] and 3-aryloxy- and alkoxy-6-arylpyridazines II [R1 = Et, C6H5, 4-FC6H4, etc.] were synthesized by an electrochem. reductive cross-coupling between chloropyridazines and aryl or heteroaryl halides. In vitro antiproliferative activity of these products I and II was evaluated against a representative panel of cancer cell lines and oncogenicity prevention of the more efficient derivatives was highlighted on human breast cancer cell line MDA-MB 468-Luc prior establishing their interaction with p44/42 and Akt-dependent signaling pathways. The highest in vitro antiproliferative activity was found for compound I [R = Et2N; Ar = 4-MeO2CC6H4] and also showed a potent ability to inhibit clonogenicity of human breast cancer cell line. The toxicity of the most active compounds I [R = Et2N; Ar = 4-MeO2CC6H4, 4-EtO2CC6H4] was further evaluated in vitro on human hepatocytes and in vivo on zebrafish assays.

Bioorganic & Medicinal Chemistry Letters published new progress about Antitumor agents. 17259-32-4 belongs to class pyridazine, name is 4-(6-Chloropyridazin-3-yl)morpholine, and the molecular formula is C8H10ClN3O, Safety of 4-(6-Chloropyridazin-3-yl)morpholine.

Referemce:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem

Crossland, Ingolf published the artcileAddition of Grignard reagents to pyridazines. X. 3-Chloro-6-dimethylaminopyridazine, Safety of 6-Chloro-N,N-dimethylpyridazin-3-amine, the main research area is pyridazines Grignard alkylation; Grignard alkylation pyridazines; alkylation Grignard pyridazines.

The reaction of 3-chloro-6-dimethylaminopyridazine with EtMgBr and PhMgBr gives 5-substituted-3-chloro-4,5-dihydro-6-dimethylaminopyridazines; the corresponding reactions with tert-BuMgBr afford 4-alkylated-4,5-dihydropyridazines. Iso-PrMgBr gives about equal amounts of the two isomers. The dihydropyridazines are identified by oxidation to the corresponding 4- or 5-substituted 3-chloro-6-dimethylaminopyridazines, which are subsequently dehalogenated and subjected to NMR anal. The results may be rationalized in terms of electronic and steric effects.

Acta Chemica Scandinavica (1947-1973) published new progress about Grignard reaction. 7145-60-0 belongs to class pyridazine, name is 6-Chloro-N,N-dimethylpyridazin-3-amine, and the molecular formula is C6H8ClN3, Safety of 6-Chloro-N,N-dimethylpyridazin-3-amine.

Referemce:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem

Albright, J. D. published the artcileSynthesis and anxiolytic activity of 6-(substituted-phenyl)-1,2,4-triazolo[4,3-b]pyridazines, Category: pyridazine, the main research area is triazolopyridazine phenyl; anxiolytic phenyltriazolopyridazine; antihypertensive phenyltriazolopyridazine; diazepam binding inhibition phenyltriazolopyridazine.

Fifty-six title compounds I (R = H, Me, Ph, etc.; R1 = H, F, Cl, NO2, etc.) were prepared in 5-92% yields starting from R1C6H4COCH2CH2CO2Et. Some I show activity in tests predictive of anxiolytic activity (protection against pentylenetetrazole-induced convulsions; thirsty rat conflict procedure). I also represent a new class of compounds which inhibit 3H-diazepam binding. Structure-activity correlations, as well as the ability of I to inhibit 3H-diazepam binding (in vitro) were discussed.

Journal of Medicinal Chemistry published new progress about Antihypertensives. 58059-33-9 belongs to class pyridazine, name is 3-Chloro-6-(3-nitrophenyl)pyridazine, and the molecular formula is C10H6ClN3O2, Category: pyridazine.

Referemce:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem

Pifferi, Giorgio published the artcileSynthesis and antihypertensive properties of new 3-hydrazinopyridazine derivatives, Safety of 6-Chloro-N,N-dimethylpyridazin-3-amine, the main research area is antihypertensive hydrazinopyridazine derivative; pyridazine hydrazino derivative antihypertensive.

Of a series of 19 title compounds substituted in the 6 position with a primary or secondary amine or an alkoxy group, several were more active than hydralazine [86-54-4] in cats as hypotensive agents and as antihypertensive agents in renal hypertensive rats. I [56393-22-7] and II [56393-23-8], prepared from 3,6-dichloropyridazine [141-30-0] by displacement of 1 Cl with the appropriate amine, followed by reaction with hydrazine and benzaldehyde, followed by hydrolysis of the hydrazone, displayed high potency and low toxicity in the tests. I reduced peripheral resistance and increased aortic, femoral, and coronary blood flow in dogs. Structure-activity relations are discussed.

Journal of Medicinal Chemistry published new progress about Antihypertensives. 7145-60-0 belongs to class pyridazine, name is 6-Chloro-N,N-dimethylpyridazin-3-amine, and the molecular formula is C6H8ClN3, Safety of 6-Chloro-N,N-dimethylpyridazin-3-amine.

Referemce:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem

Di Mola, N. published the artcilePotential antihypertensives. Synthesis of 6-substituted-N-(4H-1,2,4-triazol-4-yl)-3-pyridazinamines and 3-substituted-6-(3,5-dimethyl-1H-1,2,4-triazol-1-yl)pyridazines, SDS of cas: 17259-32-4, the main research area is pyridazinaminotriazole preparation antihypertensive; triazolylaminopyridazine preparation antihypertensive; antihypertensive dimethyltriazolylpyridazine.

A series of 6-substituted-N-(4H-1,2,4-triazol-4-yl)-3-pyridazinamines [I, R = H, Me; R1 = morpholino, piperidino, N(CH2CH2OMe)2] and 3-substituted-6-(3,5-dimethyl-1H-1,2,4-triazol-1-yl)pyridazines (II, R2 = R1, OMe, OEt, 3-tert-butyl-2-phenyl-5-oxazolidinylmethoxy, OCH2CH(OH)CH2NHCMe3, NHNH2, NHN:CHPh, 2,5-dimethylpyrrolylamino, 2,5-diethylpyrrolylamino, NHNHCO2Et) were prepared and evaluated for their oral antihypertensive activity in spontaneously hypertensive rats. Only some II induced a moderate decrease in systolic blood pressure.

Farmaco, Edizione Scientifica published new progress about Antihypertensives. 17259-32-4 belongs to class pyridazine, name is 4-(6-Chloropyridazin-3-yl)morpholine, and the molecular formula is C8H10ClN3O, SDS of cas: 17259-32-4.

Referemce:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem