Heterocyclic Building Blocks-Pyridazine

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

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

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

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

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

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

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

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

Scholz, U.; Schlummer, B. published the artcile< Arylamines>, Application In Synthesis of 20744-39-2, the main research area is review arylamine preparation organic synthesis.

A review of methods to prepare arylamines.

Science of Synthesis published new progress about Aromatic amines Role: SPN (Synthetic Preparation), PREP (Preparation). 20744-39-2 belongs to class pyridazine, and the molecular formula is C4H5N3, Application In Synthesis of 20744-39-2.

Referemce:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem

Mason, S. F. published the artcile< Frequencies and intensities of the NH stretching vibrations in primary amines>, Name: Pyridazin-4-amine, the main research area is .

The positions, extinction coefficients, and band half-widths of the symmetric and antisymmetric stretching vibration absorptions of the amide anion, and some monocyclic aliphatic, aromatic, and N-heteroaromatic primary amines were measured in the 3-μ region. Approx. values for the force constants, HHH bond angles, the “”s”” character of the hybrid orbitals bonding N to H, and the NH bond dipole gradients were calculated from the results. The force constant and the NH bond dipole gradient increase linearly with the amount of “”s”” character of the hybrid orbitals of the NH group, and in the aromatic series, these quantities increase as the π-electron charge d. on the N atom of the amino-group falls. Compound, solvent, symmetric, and antisymmetric frequency (in cm.-1) and force constant (in dyne/cm.) given: LiNH2, KBr, 3315, 3261, 5.99; cyclohexylamine, CCl4, 3381, 3316, 6.21; PhNH2, CCl4, 3481, 3395, 6.54; 2-aminopyridine (I), CCl4, 3509, 3410, 6.62; 3 analog of I, CCl4, 3481, 3396, 6.54; 4 analog of I, CCl4, 3505, 3413, 6.62; 2-aminopyrimidine (II), CCl4, 3540, 3425, 6.72; 4,6-Me2-II, CHCl3, 3533, 3422, 6.69; 4 analog of II, CCl4, 3536, 3421, 6.70; 5 analog of II, CCl4, 3485, 3399, 6.56; 2-aminopyrazine, CCl4, 3511, 3410, 6.62; 3-amino-6-methylpyridazine, CHCl3, 3509, 3407, 6.62; 4-aminopyridazine, 3514, 3415, 6.64; 3-amino-1,2,4-triazine (III), 3533, 3420, 6.70; 5,6-Me2-III, 3534, 3423, 6.68.

Journal of the Chemical Society published new progress about Amines. 20744-39-2 belongs to class pyridazine, and the molecular formula is C4H5N3, Name: Pyridazin-4-amine.

Referemce:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem