Category: 17259-32-4

Assandri, A. published the artcileMetabolic pathways of the antihypertensive agent, N-(2,5-dimethyl-1H-pyrrol-1-yl)-6-(4-morpholinyl)-3-pyridazinamine hydrochloride. I. Studies in the rat, Quality Control of 17259-32-4, the main research area is MDL 899 metabolism; pyrrolylpyridazinamine metabolism.

The metabolic fate of a new antihypertensive, MDL 899 (I) [86703-02-8] was studied in rats after both oral and i.v. administration (1 mg/kg). The compound underwent rapid metabolism, disappearing from the central compartment with a half-life of about 0.5 h. Plasma concentration of the parent drug and its major metabolite II  [100499-32-9] following i.v. and oral administration suggest a route-dependent first-pass metabolism Ten metabolites were isolated from the urine and identified by u.v., i.r., mass and 1H NMR spectroscopy. The structure of some was confirmed by 13C NMR and chem. synthesis. All biotransformations are restricted to the pyrrole ring which undergoes oxidative cleavage followed by a series of chem. rearrangements. A minor pathway leads to the formation of Me sulphinyl and Me sulfonyl pyrroles. It is suggested that, as with natural indoles, the pyrrole might be oxidized by a 2,3-dioxygenase. All metabolites tested (3 major and 2 minor) failed to showed antihypertensive activity in spontaneously hypertensive rats.

Xenobiotica published new progress about MDL 899 metabolism; pyrrolylpyridazinamine metabolism. 17259-32-4 belongs to class pyridazine, name is 4-(6-Chloropyridazin-3-yl)morpholine, and the molecular formula is C8H10ClN3O, Quality Control of 17259-32-4.

Referemce:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem

Sengmany, Stephane published the artcileAn electrochemical nickel-catalyzed arylation of 3-amino-6-chloropyridazines, Recommanded Product: 4-(6-Chloropyridazin-3-yl)morpholine, the main research area is arylaminopyridazine derivative electrochem preparation; aryl halide aminochloropyridazine electrochem arylation nickel catalyst.

3-Amino-6-aryl- and 3-amino-6-heteroarylpyridazines have been obtained in generally good yield using a nickel-catalyzed electrochem. cross-coupling between 3-amino-6-chloropyridazines and aryl or heteroaryl halides at room temperature Comparative experiments involving classical palladium-catalyzed reactions, such as Suzuki, Stille, or Negishi cross-couplings, reveal that the electrochem. method can constitute a reliable alternative tool for biaryl formation. A possible reaction mechanism is proposed on the basis of electrochem. analyses.

Journal of Organic Chemistry published new progress about Aryl halides Role: RCT (Reactant), RACT (Reactant or Reagent). 17259-32-4 belongs to class pyridazine, name is 4-(6-Chloropyridazin-3-yl)morpholine, and the molecular formula is C8H10ClN3O, Recommanded Product: 4-(6-Chloropyridazin-3-yl)morpholine.

Referemce:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem

Sengmany, Stephane published the artcileSelective mono-amination of dichlorodiazines, Recommanded Product: 4-(6-Chloropyridazin-3-yl)morpholine, the main research area is amino chloro pyridazine pyrimidine chemoselective preparation; chemoselective monosubstitution dichloropyridazine dichloropyrimidine amine triethylamine ethanol; kinetics relative reactivity chemoselective monosubstitution dichloropyridazine dichloropyrimidine morpholine.

3,6-Dichloropyridazine, 4,6-dichloropyrimidine, 2,4-dichloropyrimidine, and 3,5-dichloropyridazine underwent chemoselective monosubstitution reactions with amines using triethylamine as a base in ethanol at either ambient temperature or reflux to give monoamino monochloro pyridazines and pyrimidines. The methodol. is general and efficient despite noticeable differences in reactivity between diazines; while dichloropyridazine and dichloropyrazine require several hours of heating at reflux for the reaction to proceed, dichloropyrimidines reach completion within minutes at room temperature

Tetrahedron published new progress about Amines Role: RCT (Reactant), RACT (Reactant or Reagent). 17259-32-4 belongs to class pyridazine, name is 4-(6-Chloropyridazin-3-yl)morpholine, and the molecular formula is C8H10ClN3O, Recommanded Product: 4-(6-Chloropyridazin-3-yl)morpholine.

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

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

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

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

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

Matulenko, Mark A. published the artcile4-Amino-5-aryl-6-arylethynylpyrimidines: Structure-activity relationships of non-nucleoside adenosine kinase inhibitors, Synthetic Route of 17259-32-4, the main research area is aminoarylarylethynylpyrimidine derivative preparation structure adenosine kinase inhibitor analgesic pain.

A series of nonnucleoside adenosine kinase (AK) inhibitors is reported. These inhibitors originated from the modification of 5-(3-bromophenyl)-7-(6-morpholin-4-ylpyridin-3-yl)pyrido[2,3-d]pyrimidin-4-ylamine (ABT-702). The identification of a linker that would approx. the spatial arrangement found between the pyrimidine ring and the aryl group at C(7) in ABT-702 was a key element in this modification. A search of potential linkers led to the discovery of an acetylene moiety as a suitable scaffold. It was hypothesized that the aryl acetylenes, ABT-702, and adenosine bound to the active site of AK (closed form) in a similar manner with respect to the orientation of the heterocyclic base. Although potent acetylene analogs were discovered based on this assumption, an x-ray crystal structure of 5-(4-dimethylaminophenyl)-6-(6-morpholin-4-ylpyridin-3-ylethynyl)pyrimidin-4-ylamine (I) revealed a binding orientation contrary to adenosine. In addition, this compound bound tightly to a unique open conformation of AK. The structure-activity relationships and unique ligand orientation and protein conformation are discussed.

Bioorganic & Medicinal Chemistry 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, Synthetic Route of 17259-32-4.

Referemce:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem