Month: November 2022

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

Steck, Edgar A. published the artcilePyridazines. VIII. 6-Aryl-3-(basically substituted) pyridazines, Safety of 3-Chloro-6-(3-nitrophenyl)pyridazine, the main research area is pyridazine phenylaminoethoxy; aminoethoxypyridazine; chloropyridazine substitution aminoethanol putrescine; cyclization chloropyridazine aminoethylphenethylamine; pyrrolidinopyridazine.

Substitution reaction of the chloropyridazines I [R = 4-ClC6H4, 3,4-Cl2C6H3, 4-MeOC6H4, 3,4-Br(MeO)C6H3, 3-O2NC6H4, 2-thienyl, 5-bromo-2-thienyl] with R1H [R1 = Et2NCH2CH2O, Et2NCH2CH2CH2CHMeNH, Et2NCH2CH(OH)CH2NH, NH2, Me2N] gave the pyridazines II. I (R = 4-ClC6H4, 3,4-Cl2C6H3) with Et2NCH2CH2CH(C6H4Cl-4)CH2NH2 also gave the pyrrolidinopyridazines III, and I (R = 4-MeOC6H4) with Et2N(CH2)3CHMeNH2 in a phenol melt at 160-5° gave 5-(diethylamino)-N,N-bis[6-(4-methoxyphenyl)-3-pyridazinyl]-2-pentylamine.

Journal of Heterocyclic Chemistry published new progress about Substitution reaction. 58059-33-9 belongs to class pyridazine, name is 3-Chloro-6-(3-nitrophenyl)pyridazine, and the molecular formula is C10H6ClN3O2, Safety of 3-Chloro-6-(3-nitrophenyl)pyridazine.

Referemce:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem

Xu, Qile published the artcileSynthesis and Bioevaluation of 3,6-Diaryl-[1,2,4]triazolo[4,3-b] Pyridazines as Antitubulin Agents, Name: 3-Chloro-6-(3-nitrophenyl)pyridazine, the main research area is triazolo pyridazine preparation antitubulin antiproliferative activity SAR; [1,2,4]Triazolo[4,3-b]pyridazine; colchicine binding site; combretastatin A-4; molecular modeling; tubulin.

A series of 3,6-diaryl-[1,2,4]triazolo[4,3-b]pyridazines were designed as a class of vinylogous CA-4 analogs. The easily isomerized (Z,E)-butadiene linker of vinylogous CA-4 was replaced by a rigid [1,2,4]triazolo[4,3-b]pyridazine scaffold. Twenty-one target compounds were synthesized and exhibited moderate to potent antiproliferative activity. The compound with a 3-amino-4-methoxyphenyl moiety as the B-ring, comparable to CA-4 (IC50 = 0.009-0.012 μM), displayed the highly active antiproliferative activity against SGC-7901, A549, and HT-1080 cell lines with IC50 values of 0.014, 0.008, and 0.012 μM, resp. Tubulin polymerization experiments indicated that it effectively inhibited tubulin polymerization, and immunostaining assay revealed that it significantly disrupted tubulin microtubule dynamics. Moreover, cell cycle studies revealed that this compound dramatically arrested cell cycle progression at G2/M phase in A549 cells. Mol. modeling studies showed that it could bind to the colchicine binding site on microtubules.

ACS Medicinal Chemistry Letters published new progress about Antiproliferative agents. 58059-33-9 belongs to class pyridazine, name is 3-Chloro-6-(3-nitrophenyl)pyridazine, and the molecular formula is C10H6ClN3O2, Name: 3-Chloro-6-(3-nitrophenyl)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

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

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

Ibrahim, Tamer H. published the artcileSynthesis of Some Novel 2,6-Disubstituted Pyridazin-3(2H)-one Derivatives as Analgesic, Anti-Inflammatory, and Non-Ulcerogenic Agents, Formula: C6H8ClN3, the main research area is alkyl phenoxypyridazinone preparation analgesic antiinflammatory ulcerogenic cyclooxygenase inhibitor SAR; benzyl aminopyridazinone preparation analgesic antiinflammatory ulcerogenic cyclooxygenase inhibitor SAR; aralkyl pyrazolylpyridazinone preparation analgesic antiinflammatory ulcerogenic cyclooxygenase inhibitor SAR; Analgesic activity; Anti-inflammatory; COX-1; COX-2; Pyridazinone.

Some novel 2,6-disubstituted pyridazine-3(2H)-one derivatives I [R1 = p-tolyl, benzyl, 2,6-di-MeC6H3, etc; R2 = Et, Ph, 4-Br-C6H4, phthalimido; X = N, O] and II [R3 = Ph, 4-Br-C6H4, phthalimido] were synthesized and evaluated for in-vitro cyclooxygenase-2 (COX-2) inhibitory efficacy. Compounds I [R1 = o-tolyl, R2 = phthalimido, X = O; R1 = o-tolyl, R2 = Et, X = O] and II [R3 = Ph] showed the most potent COX-2 inhibitory activity with IC50 values of 0.19, 0.11, and 0.24 μM, resp. The synthesized compounds with the highest COX-2 selectivity indexes were evaluated for their anti-inflammatory, analgesic, and ulcerogenic activities. Compounds I [R1 = o-tolyl, R2 = Et, X = O] and II [R3 = Ph] demonstrated the most potent and consistent anti-inflammatory activity over the synthesized compounds, which was significantly higher than that of celecoxib in the carrageenin rat paw edema model and with milder ulcer scoring than that of indomethacin in the ulcerogenicity screening.

Archiv der Pharmazie (Weinheim, Germany) published new progress about Analgesics. 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