Tag: M.W=150-200

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

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

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

Beinat, Corinne published the artcileStructure-activity relationship studies of SEN12333 analogues: Determination of the optimal requirements for binding affinities at α7 nAChRs through incorporation of known structural motifs, Category: pyridazine, the main research area is structure cognition enhancer preparation acetylcholine receptor; Acetylcholine receptor; CNS; Structure–activity relationships; α7 nicotinic receptors.

Alpha7 nicotinic acetylcholine receptors (nAChRs) have implications in the regulation of cognitive processes such as memory and attention and have been identified as a promising therapeutic target for the treatment of the cognitive deficits associated with schizophrenia and Alzheimer’s disease (AD). Structure affinity relationship studies of the previously described α7 agonist SEN12333, have resulted in the identification of compound I, a potent and selective agonist of the α7 nAChR with enhanced affinity and improved physicochem. properties over the parent compound (SEN12333).

European Journal of Medicinal Chemistry published new progress about Cognition enhancers. 17259-32-4 belongs to class pyridazine, name is 4-(6-Chloropyridazin-3-yl)morpholine, and the molecular formula is C8H10ClN3O, Category: pyridazine.

Referemce:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem

Lee, Woo published the artcileReaction of chloropyridazines with N,N-dimethylformamide, Formula: C6H8ClN3, the main research area is pyridazine dimethylamino preparation; chloropyridazine amination regioselective DMF.

Chloropyridazine derivatives were reacted with DMF under reflux conditions to give the corresponding (N,N-dimethylamino)pyridazines regioselectively. E.g., amination of 3,6-dichloropyridazine with refluxing DMF gave 95% 6-chloro-3-(dimethylamino)pyridazine. In some cases, the addition of powd. Cu as catalyst was necessary.

Journal of Heterocyclic Chemistry published new progress about Amination, regioselective. 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

Turner, Christopher J. published the artcileChlorine-35 nuclear quadrupole resonance spectra of chlorodiazines, Recommanded Product: 6-Chloro-N,N-dimethylpyridazin-3-amine, the main research area is chlorine NQR azine.

Comparison of observed and calculated 35Cl NQR data for 17 chloroazines showed it is not possible to extrapolate from chloropyridine to chlorodiazines since the effect of the addnl. N is mainly inductive rather than conjugative. Large solid-state splittings were observed in some chloropyridazines.

Journal of the Chemical Society, Perkin Transactions 8: Physical Organic Chemistry published new progress about Nuclear quadrupole resonance. 7145-60-0 belongs to class pyridazine, name is 6-Chloro-N,N-dimethylpyridazin-3-amine, and the molecular formula is C6H8ClN3, Recommanded Product: 6-Chloro-N,N-dimethylpyridazin-3-amine.

Referemce:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem

Lewis, Susan J. published the artcileRationalizations among heterocyclic partition coefficients. Part 2: The azines, Recommanded Product: 6-Chloro-N,N-dimethylpyridazin-3-amine, the main research area is azine structure partition coefficient; LFER azine.

π-Values (partition substituent constants) of 246 azines are given and discussed in terms of Δπ, the difference in π-value from that expected for C6H6. It is shown that Δπ is close to zero for alkyl and most halogen groups, but for polar substituents capable of H bonding it may be as high as φ1.6. Except for peri-positions, these Δπ-values may be correlated by a set of equations specific for different types of substituent position and containing terms which sep. parameterize proton-donor and -acceptor ability. The rationale behind this treatment is justified in terms of the nature of the octanol-H2O partitioning process and the manner in which electronic effects are expected to operate, in this context and that of the individual mol. Other topics discussed include: reasons for deviations among “”irregular”” substituents; the special problems of peri-positions; multisubstitution; and some consequences of this anal. for other types of compound

Quantitative Structure-Activity Relationships published new progress about Molecular structure-property relationship, partition. 7145-60-0 belongs to class pyridazine, name is 6-Chloro-N,N-dimethylpyridazin-3-amine, and the molecular formula is C6H8ClN3, Recommanded Product: 6-Chloro-N,N-dimethylpyridazin-3-amine.

Referemce:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem