Category: pyridazine

Bosset, Cyril; Beucher, Helene; Bretel, Guillaume; Pasquier, Elisabeth; Queguiner, Laurence; Henry, Cyril; Vos, Ann; Edwards, James P.; Meerpoel, Lieven; Berthelot, Didier published the artcile< Minisci-Photoredox-Mediated α-Heteroarylation of N-Protected Secondary Amines: Remarkable Selectivity of Azetidines>, Safety of Ethyl 6-chloroimidazo[1,2-b]pyridazine-2-carboxylate, the main research area is Minisci photoredox mediated alpha heteroarylation azetidine; heteroarylation azetidine spirocyclic derivative.

The development of a general, mild, and functional-group-tolerant direct functionalization of N-heteroarenes by C-H functionalization with N-protected amines, including azetidines under Minisci-mediated photoredox conditions, is reported. A broad scope of substituted azetidines, including spirocyclic derivatives, and heterocycles were explored. This reaction enables the production of sp3-rich complex druglike structures in one step from unactivated feedstock amines and heterocycles.

Organic Letters published new progress about Azetidines Role: RCT (Reactant), SPN (Synthetic Preparation), RACT (Reactant or Reagent), PREP (Preparation). 64067-99-8 belongs to class pyridazine, and the molecular formula is C9H8ClN3O2, Safety of Ethyl 6-chloroimidazo[1,2-b]pyridazine-2-carboxylate.

Referemce:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem

Ding, Xiao; Dai, Xuedong; Long, Kai; Peng, Cheng; Andreotti, Daniele; Bamborough, Paul; Eatherton, Andrew J.; Edge, Colin; Jandu, Karamjit S.; Nichols, Paula L.; Philps, Oliver J.; Stasi, Luigi Piero; Wan, Zehong; Xiang, Jia-Ning; Dong, Kelly; Dossang, Pamela; Ho, Ming-Hsun; Li, Yi; Mensah, Lucy; Guan, Xiaoming; Reith, Alastair D.; Ren, Feng published the artcile< Discovery of 5-substituent-N-arylbenzamide derivatives as potent, selective and orally bioavailable LRRK2 inhibitors>, Name: Pyridazin-4-amine, the main research area is arylbenzamide synthesis SAR pharmacokinetics LRRK2 Parkinson disease; Arylbenzamide; CNS penetration; Kinase selectivity; LRRK2 inhibitor; Parkinson’s disease.

Leucine-rich repeat kinase 2 (LRRK2) has been suggested as a potential therapeutic target for Parkinson’s disease. Herein we report the discovery of 5-substituent-N-arylbenzamide derivatives as novel LRRK2 inhibitors. Extensive SAR study led to the discovery of compounds I, which demonstrated potent LRRK2 inhibition activity, high selectivity across the kinome, good brain exposure, and high oral bioavailability.

Bioorganic & Medicinal Chemistry Letters published new progress about Antiparkinsonian agents. 20744-39-2 belongs to class pyridazine, and the molecular formula is C4H5N3, Name: Pyridazin-4-amine.

Referemce:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem

Russell, Michael G. N.; Carling, Robert W.; Atack, John R.; Bromidge, Frances A.; Cook, Susan M.; Hunt, Peter; Isted, Catherine; Lucas, Matt; McKernan, Ruth M.; Mitchinson, Andrew; Moore, Kevin W.; Narquizian, Robert; Macaulay, Alison J.; Thomas, David; Thompson, Sally-Anne; Wafford, Keith A.; Castro, Jose L. published the artcile< Discovery of Functionally Selective 7,8,9,10-Tetrahydro-7,10-ethano-1,2,4-triazolo[3,4-a]phthalazines as GABAA Receptor Agonists at the α3 Subunit>, Formula: C5H4Cl2N2, the main research area is triazolophthalazine tetrahydroethano preparation human GABA receptor agonist acidity.

7,8,9,10-Tetrahydro-7,10-ethano-1,2,4-triazolo[3,4-a]phthalazine I (R1 = Ph; R2 = 2-pyridylmethyl) was previously identified as a potent partial agonist for the α3 receptor subtype with 5-fold selectivity in binding affinity over α1. This paper describes a detailed investigation of the substituents on this core structure at both the 3- and 6-positions. Despite evaluating a wide range of groups, the maximum selectivity that could be achieved in terms of affinity for the α3 subtype over the α1 subtype was 12-fold (for I [R1 = Ph; R2 = 4-(HOCH2)C6H4CH2]). Although most analogs showed no selectivity in terms of efficacy, some of them, e.g. I (R1 = Ph; R2 = 3,5-dimethyl-2-pyridylmethyl, pyrazol-1-ylmethyl), did show partial agonism at α1 and antagonism at α3. However, two analogs I (R1 = Ph; R2 = 1-methyl-1,2,4-triazol-3-ylmethyl, 2-propyl-1,2,4-triazol-3-ylmethyl), containing triazole substituents in the 6-position, showed significantly higher efficacy for the α3 subtype over the α1 subtype. This was the first indication that selectivity in efficacy in the required direction could be achieved in this series.

Journal of Medicinal Chemistry published new progress about Acidity. 120276-59-7 belongs to class pyridazine, and the molecular formula is C5H4Cl2N2, Formula: C5H4Cl2N2.

Referemce:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem

Jiang, Li-wen published the artcile< Analysis of volatile substances from Psophocarpus tetragonolobus D. C. seeds>, Name: Pyridazin-4-amine, the main research area is volatile substance Psophocarpus seed.

Objective: To analyze volatile substances from Psophocarpus tetragonolobus D. C seeds, so as to provide a basis to make better use of this resources. Method: Volatile substances extracted from Psophocarpus tetragonolobus D. C seeds were identified by GC-MS, and their relative contents were determined through area normalization method. Result: 125 kinds of compounds in 10 types including alkanes, olefine, acids, aromatic compounds, esters, ketone, ethers and heterlcyclic series were identified from 4 Psophocarpus tetragonolobus D. C seeds. Moreover each kind of seeds had 42 volatile substances mainly referred to ketone, alc. and esters. There was no significant difference regarding types and total amount of volatile substances from Psophocarpus tetragonolobus D. C seeds among different species, but their relative contents were differed obviously. Conclusion: The existence and differences of volatile substances formed their own characteristic flavors that could contribute to products variation in the processing of Psophocarpus tetragonolobus D. C.

Anhui Nongye Kexue published new progress about Psophocarpus tetragonolobus. 20744-39-2 belongs to class pyridazine, and the molecular formula is C4H5N3, Name: Pyridazin-4-amine.

Referemce:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem

Ahmed, Mais Emad; Jawad, Neam Hadier; Al-Shimmary, Sana MH; Basi, Rabaab Qzar published the artcile< Isolation and identification multidrug resistance bacteria from urinary tract infectious and effect of Capsicum Annuum oil>, Category: pyridazine, the main research area is pepper essential oil urine tract infection antimicrobial.

This study was done to assess the proliferation bacterial and susceptibility resistance antibiotic pattern of (UTIs) pathogens. For identification of mid stream urine samples 40 causative microbial agents from 10-50 years clin. sample with clin. symptoms to be UTI were collected and appropriate biochem. tests. These samples were collected from Teaching Laboratories Center in Baghdad. The antimicrobial sensitivity test was carried out by Well Diffusion Assay technique using Muller-Hinton agar. Overall female only the most isolates were Escherichia coli with average rate of 50% followed by Enterobacter spp. (12%). Whereas, Klebsiella, Pseudomonas Aeruginosa and Enter occurs faecalis showed frequency rate of 9% for each. (Family Solanaceae) species Capsicum frutescent L. Usually used most of the spice, (red peppers) is also increased benefits with multiple healths human. In the study, yield extract included constituents phytochem. of (n-hexane, chloroform, Et acetate, acetone and methanol) extracts of dried fruit. Antibacterial activity in vitro of extracts was determined by WADA method gram pos. bacteria (Staphylococcus Aureus) and gram neg. bacteria (Escherichia coli, Pseudomonas Aeruginosa, Klebsiella pneumonia and Enterococcus faecalis). MIC evaluated by two fold serial broth tube dilution method ranged between 0.312 to 5 mg/mL.

Research Journal of Pharmaceutical, Biological and Chemical Sciences published new progress about Antibacterial agents. 20744-39-2 belongs to class pyridazine, and the molecular formula is C4H5N3, Category: pyridazine.

Referemce:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem

Venturello, P.; Barbero, M. published the artcile< Product subclass 6: potassium amides and phosphides>, Related Products of 20744-39-2, the main research area is review potassium amide organic synthesis; potassium phosphide organic synthesis review.

A review of the application of potassium amides and phosphides to organic synthesis.

Science of Synthesis published new progress about Organic synthesis. 20744-39-2 belongs to class pyridazine, and the molecular formula is C4H5N3, Related Products of 20744-39-2.

Referemce:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem

Hara, Hiroshi; Van der Plas, Henk C. published the artcile< On the amination of azaheterocycles. A new procedure for the introduction of an amino group>, Recommanded Product: Pyridazin-4-amine, the main research area is amination azaheterocycle; heterocycle aza amination; diazine amination; triazine amination; pyrimidine amination; pyridazine amination.

Diazines and triazines were aminated using KNH2, liquid NH3 and KMnO4. Thus, 4-aminopyridazine was obtained in 91% yield from pyridazine.

Journal of Heterocyclic Chemistry published new progress about Amination. 20744-39-2 belongs to class pyridazine, and the molecular formula is C4H5N3, Recommanded Product: Pyridazin-4-amine.

Referemce:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem

Venkatesan, Aranapakam M.; Chen, Zecheng; Dos Santos, Osvaldo; Dehnhardt, Christoph; Santos, Efren Delos; Ayral-Kaloustian, Semiramis; Mallon, Robert; Hollander, Irwin; Feldberg, Larry; Lucas, Judy; Yu, Ker; Chaudhary, Inder; Mansour, Tarek S. published the artcile< PKI-179: an orally efficacious dual phosphatidylinositol-3-kinase (PI3K)/mammalian target of rapamycin (mTOR) inhibitor>, Electric Literature of 20744-39-2, the main research area is substituted triazine derivative preparation PI3K mTOR inhibitor.

A series of mono-morpholino 1,3,5-triazine derivatives bearing a 3-oxa-8-azabicyclo[3.2.1]octane were prepared and evaluated for PI3-kinase/mTOR activity. Replacing one of the bis-morpholines in lead compound I (PKI-587) with 3-oxa-8-azabicyclo[3.2.1]octane and reducing the mol. weight led to compound II (PKI-179), an orally efficacious dual PI3-kinase/mTOR inhibitor. The in vitro activity, in vivo efficacy, and PK properties of II are discussed.

Bioorganic & Medicinal Chemistry Letters published new progress about Enzyme inhibitors. 20744-39-2 belongs to class pyridazine, and the molecular formula is C4H5N3, Electric Literature of 20744-39-2.

Referemce:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem

Yuan, Xinrui; Wu, Hanshu; Bu, Hong; Zheng, Peiyuan; Zhou, Jinpei; Zhang, Huibin published the artcile< Design, synthesis and biological evaluation of pyridone-aminal derivatives as MNK1/2 inhibitors>, Recommanded Product: Pyridazin-4-amine, the main research area is pyridone aminal derivative preparation MNK1 MNK2 inhibitor colon cancer; MNK1/2; Pyridone–aminal; eFT508; eIF4E.

Excessive phosphorylation of eukaryotic translation initiation factor 4E (eIF4E) plays a major role in the dysregulation of mRNA translation and the activation of tumor cell signaling. eIF4E is exclusively phosphorylated by mitogen-activated protein kinase interacting kinases 1 and 2 (MNK1/2) on Ser209. So, MNK1/2 inhibitors could decrease the level of p-eIF4E and regulate tumor-associated signaling pathways. A series of pyridone-aminal derivatives were synthesized and evaluated as MNK1/2 inhibitors. Several compounds exhibited great inhibitory activity against MNK1/2 and selected compounds showed moderate to excellent anti-proliferative potency against hematol. cancer cell lines. In particular, compound 42i (MNK1 IC50 = 7.0 nM; MNK2 IC50 = 6.1 nM) proved to be the most potent compound against TMD-8 cell line with IC50 value of 0.91 μM. Furthermore, 42i could block the phosphorylation level of eIF4E in CT-26 cell line, and 42i inhibited the tumor growth of CT-26 allograft model significantly. These results indicated that compound 42i was a promising MNK1/2 inhibitor for the potent treatment of colon cancer.

Bioorganic & Medicinal Chemistry published new progress about Antiproliferative agents. 20744-39-2 belongs to class pyridazine, and the molecular formula is C4H5N3, Recommanded Product: Pyridazin-4-amine.

Referemce:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem

Zhao, Hong; Jin, Jian published the artcile< Visible Light-Promoted Aliphatic C-H Arylation Using Selectfluor as a Hydrogen Atom Transfer Reagent>, COA of Formula: C9H8ClN3O2, the main research area is alkane heteroarene selectfluor hydrogen atom transfer light arylation; heteroaryl alkyl derivative preparation.

A mild, practical method for direct arylation of unactivated C(sp3)-H bonds with heteroarenes has been achieved via photochem. Selectfluor is used as a hydrogen atom transfer reagent under visible light irradiation A diverse range of chem. feedstocks, such as alkanes, ketones, esters, and ethers, and complex mols. readily undergo intermol. C(sp3)-C(sp2) bond formation. Moreover, a broad array of heteroarenes, including pharmaceutically useful scaffolds, can be alkylated effectively by the protocol presented here.

Organic Letters published new progress about Alkanes Role: RCT (Reactant), RACT (Reactant or Reagent). 64067-99-8 belongs to class pyridazine, and the molecular formula is C9H8ClN3O2, COA of Formula: C9H8ClN3O2.

Referemce:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem