Tag: 95.1026

Cu-Catalyzed Aerobic Oxidative Cyclization of Guanidylpyridines and Derivatives was written by Bartels, Bjorn;Bolas, Conor Gordon;Cueni, Philipp;Fantasia, Serena;Gaeng, Nicolas;Trita, Andrada Stefania. And the article was included in Journal of Organic Chemistry in 2015.Synthetic Route of C4H5N3 This article mentions the following:

A new method for the straightforward synthesis of 2-amino-[1,2,4]triazolo[1,5-a]pyridines and derivatives is presented. The target products are synthesized in high yields from guanidylpyridines and analogs via copper-catalyzed N-N coupling. The present methodol. shows a wide scope, tolerating not only different substituents on the pyridine ring but also different heterocylic rings such as pyrazines, pyrimidines, and pyridazines. In the experiment, the researchers used many compounds, for example, 3-Aminopyridazine (cas: 5469-70-5Synthetic Route of C4H5N3).

3-Aminopyridazine (cas: 5469-70-5) belongs to pyridazine derivatives. Pyridazines is a six-membered nitrogen-containing significant heterocycle. It has received considerable interest because of its useful applications as natural products, pharmaceuticals, and various bioactive molecules. Specifically, the pyridazine moiety is an important structural feature of various pharmacologically important compounds with activities like antimicrobial, analgesic, anti-inflammatory, antiplatelet, anticancer, antisecretory, antiulcer, antidepressant, cardiotonic, vasodilator, antiarrhythmic, and hypocholesterolaemic.Synthetic Route of C4H5N3

Referemce:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem

Ultrasonicated synthesis of N-benzyl-2,3-substituted morpholines, via the Mitsunobu diol cyclisation was written by Reddy, B. Jayachandra;Reddy, M. C. Somasekhara. And the article was included in E-Journal of Chemistry in 2010.Name: 3-Aminopyridazine This article mentions the following:

A facile five-step synthesis of N-benzyl-2,3-substituted morpholines was performed. The key steps were microwave-assisted Friedel-Crafts acylation and diol cyclization carried out via an ultra sonication of Mitsunobu reaction using diethylazodicarboxylate, TPP in THF for 1 h. The morpholine products were generated as diastereomers which was separated by the column chromatog. in yields. The structure of compounds was characterized by the spectral data. In the experiment, the researchers used many compounds, for example, 3-Aminopyridazine (cas: 5469-70-5Name: 3-Aminopyridazine).

3-Aminopyridazine (cas: 5469-70-5) belongs to pyridazine derivatives. Pyridazine-based compounds continued to be a great source of biologically active compounds as evidenced by the number of publications which emerged in 2021. Specifically, the pyridazine moiety is an important structural feature of various pharmacologically important compounds with activities like antimicrobial, analgesic, anti-inflammatory, antiplatelet, anticancer, antisecretory, antiulcer, antidepressant, cardiotonic, vasodilator, antiarrhythmic, and hypocholesterolaemic.Name: 3-Aminopyridazine

Referemce:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem

Sulfonamides as Selective Na_V1.7 Inhibitors: Optimizing Potency and Pharmacokinetics While Mitigating Metabolic Liabilities was written by Weiss, Matthew M.;Dineen, Thomas A.;Marx, Isaac E.;Altmann, Steven;Boezio, Alessandro;Bregman, Howard;Chu-Moyer, Margaret;DiMauro, Erin F.;Feric Bojic, Elma;Foti, Robert S.;Gao, Hua;Graceffa, Russell;Gunaydin, Hakan;Guzman-Perez, Angel;Huang, Hongbing;Huang, Liyue;Jarosh, Michael;Kornecook, Thomas;Kreiman, Charles R.;Ligutti, Joseph;La, Daniel S.;Lin, Min-Hwa Jasmine;Liu, Dong;Moyer, Bryan D.;Nguyen, Hanh N.;Peterson, Emily A.;Rose, Paul E.;Taborn, Kristin;Youngblood, Beth D.;Yu, Violeta;Fremeau, Robert T.. And the article was included in Journal of Medicinal Chemistry in 2017.Recommanded Product: 3-Aminopyridazine This article mentions the following:

Several reports have recently emerged regarding the identification of heteroarylsulfonamides as Na_V1.7 inhibitors that demonstrate high levels of selectivity over other Na_V isoforms. The optimization of a series of internal Na_V1.7 leads that address a number of metabolic liabilities including bioactivation, PXR activation, as well as CYP3A4 induction and inhibition led to the identification of potent and selective inhibitors that demonstrated favorable pharmacokinetic profiles and were devoid of the aforementioned liabilities. The key to achieving this within a series prone to transporter-mediated clearance was the identification of a small range of optimal cLogD values and the discovery of subtle PXR SAR that was not lipophilicity dependent. This enabled the identification of compound 20, which was advanced into a target engagement pharmacodynamic model where it exhibited robust reversal of histamine-induced scratching bouts in mice. In the experiment, the researchers used many compounds, for example, 3-Aminopyridazine (cas: 5469-70-5Recommanded Product: 3-Aminopyridazine).

3-Aminopyridazine (cas: 5469-70-5) belongs to pyridazine derivatives. The pyridazine derivatives are mostly present in biologically active compounds and are also present with different pharmacophores. Pyridazine is bioavailable (especially in the CNS) and can reduce toxicity. Pyridazine is a component of several drug molecules, and the pyridazine pharmacophore has contributed to a variety of pharmacologically active compounds.Recommanded Product: 3-Aminopyridazine

Referemce:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem

Synthesis of polyfunctional fluoro-quinoline and fluoro-pyridopyrimidinone derivatives was written by Heeran, Darren;Murray, Ben J.;Qiu, Sili;Martin, Sophie J.;Skelton, Robert M.;Dodds, Kiera R.;Yufit, Dmitry S.;Sandford, Graham. And the article was included in Journal of Fluorine Chemistry in 2021.Electric Literature of C4H5N3 This article mentions the following:

2-Fluoromalonic acid is a useful building block for the synthesis of selectively fluorinated heterocycles. In the presence of phosphoryl chloride, chlorinated fluoroquinolines and fluoro-pyridopyrimidinones were prepared in a single step by an efficient tandem chlorination-cyclisation process. Functionalisation by Suzuki cross-coupling or S_NAr processes allowed for the rapid construction of a small library of 30 novel polysubstituted selectively fluorinated quinoline and pyridopyrimidinone derivatives in high yields and bearing a diverse range of substituents. In the experiment, the researchers used many compounds, for example, 3-Aminopyridazine (cas: 5469-70-5Electric Literature of C4H5N3).

3-Aminopyridazine (cas: 5469-70-5) belongs to pyridazine derivatives. The pyridazine structure is a popular pharmacophore which is found within a number of herbicides such as credazine, pyridafol and pyridate. Pyridazine and derivatives coordinate readily with transition metals to form complexes and catalysts with synthetic utility.Electric Literature of C4H5N3

Referemce:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem

Electronic structure and spectra of organic molecules. XVI. Amine-imine tautomerism in azines substituted by amino groups was written by Kwiatkowski, J. S.. And the article was included in Acta Physica Polonica, A in 1972.Recommanded Product: 3-Aminopyridazine This article mentions the following:

For both amine and imine tautomers of amine-substituted pyridines and diazines, Pariser-Parr-Pople type calculations (K., 1970) gave singlet-singlet transition energies which agreed with exptl. data. In all cases, the singlet-singlet transitions of the imine forms red shifted relative to the corresponding transitions of the amine forms. In the experiment, the researchers used many compounds, for example, 3-Aminopyridazine (cas: 5469-70-5Recommanded Product: 3-Aminopyridazine).

3-Aminopyridazine (cas: 5469-70-5) belongs to pyridazine derivatives. The pyridazine structure is a popular pharmacophore which is found within a number of herbicides such as credazine, pyridafol and pyridate. Pyridazine compounds have attracted interest in various fields like medicinal, industrial, and agricultural research as they are used for numerous biological activities and other applications.Recommanded Product: 3-Aminopyridazine

Referemce:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem

Discovery and Characterization of Selective and Ligand-Efficient DYRK Inhibitors was written by Henderson, Scott H.;Sorrell, Fiona;Bennett, James;Fedorov, Oleg;Hanley, Marcus T.;Godoi, Paulo H.;Ruela de Sousa, Roberta;Robinson, Sean;Ashall-Kelly, Alexander;Hopkins Navratilova, Iva;Walter, Daryl S.;Elkins, Jonathan M.;Ward, Simon E.. And the article was included in Journal of Medicinal Chemistry in 2021.Formula: C4H5N3 This article mentions the following:

Dual-specificity tyrosine-regulated kinase 1A (DYRK1A) regulates the proliferation and differentiation of neuronal progenitor cells during brain development. Consequently, DYRK1A has attracted interest as a target for the treatment of neurodegenerative diseases, including Alzheimer’s disease (AD) and Down’s syndrome. Recently, the inhibition of DYRK1A has been investigated as a potential treatment for diabetes, while DYRK1A’s role as a mediator in the cell cycle has garnered interest in oncol. indications. Structure-activity relationship (SAR) anal. in combination with high-resolution X-ray crystallog. leads to a series of pyrazolo[1,5-b]pyridazine inhibitors with excellent ligand efficiencies, good physicochem. properties, and a high degree of selectivity over the kinome. Compound 11 (I) exhibited good permeability and cellular activity without P-glycoprotein liability, extending the utility of 11 in an in vivo setting. These pyrazolo[1,5-b]pyridazines are a viable lead series in the discovery of new therapies for the treatment of diseases linked to DYRK1A function. In the experiment, the researchers used many compounds, for example, 3-Aminopyridazine (cas: 5469-70-5Formula: C4H5N3).

3-Aminopyridazine (cas: 5469-70-5) belongs to pyridazine derivatives. The pyridazine derivatives are mostly present in biologically active compounds and are also present with different pharmacophores. Pyridazine can act as a hydrogen bond acceptor to improve the physicochemical properties of drug molecules by increasing their water solubility, and has a high affinity for complexing with targets due to its dipole moment.Formula: C4H5N3

Referemce:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem

A rhodamine-based fluorescent probe for Fe³⁺: synthesis, theoretical calculation and bioimaging application was written by Cheng, Zhao;Zheng, Lei;Xu, Hao;Pang, Long;He, Hao. And the article was included in Analytical Methods in 2019.Quality Control of 3-Aminopyridazine This article mentions the following:

A novel rhodamine-based fluorescent probe was designed and synthesized. Its metal ion selectivity was illuminated by the highly specific recognition of the probe towards Fe³⁺ over other metal ions; moreover, the color change in the recognition process of Fe3+ could be used for its “naked-eye” detection in an aqueous environment. In addition, a theor. calculation was performed to reveal the possible reaction mechanism between the probe and Fe³⁺. The fluorescent imaging of Fe³⁺ in living cells further suggested future applications of the probe for instant Fe³⁺ detection in a clin. diagnosis and dynamic tracking of Fe³⁺ in biol. systems. In the experiment, the researchers used many compounds, for example, 3-Aminopyridazine (cas: 5469-70-5Quality Control of 3-Aminopyridazine).

3-Aminopyridazine (cas: 5469-70-5) belongs to pyridazine derivatives. The pyridazine derivatives are mostly present in biologically active compounds and are also present with different pharmacophores. Pyridazine compounds have attracted interest in various fields like medicinal, industrial, and agricultural research as they are used for numerous biological activities and other applications.Quality Control of 3-Aminopyridazine

Referemce:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem

Synthesis of peptide nucleic acids containing pyridazine derivatives as cytosine and thymine analogs, and their duplexes with complementary oligodeoxynucleotides was written by Tomori, Takahito;Miyatake, Yuya;Sato, Yuta;Kanamori, Takashi;Masaki, Yoshiaki;Ohkubo, Akihiro;Sekine, Mitsuo;Seio, Kohji. And the article was included in Organic Letters in 2015.Application In Synthesis of 3-Aminopyridazine This article mentions the following:

Synthesis of peptide nucleic acids (PNAs) is reported with new pyridazine-type nucleobases: 3-aminopyridazine (aPz) and 1-aminophthalazine (aPh) as cytosine analogs, and pyridazin-3-one (Pz^O) and phthalazin-1-one (Ph^O) as thymine analogs. The PNAs having an aPz or a Pz^O formed duplexes with each complementary oligodeoxynucleotide forming a base pair with G or A, resp., as evaluated by using UV melting analyses and CD (CD) spectra. In the experiment, the researchers used many compounds, for example, 3-Aminopyridazine (cas: 5469-70-5Application In Synthesis of 3-Aminopyridazine).

3-Aminopyridazine (cas: 5469-70-5) belongs to pyridazine derivatives. Pyridazine-based compounds continued to be a great source of biologically active compounds as evidenced by the number of publications which emerged in 2021. The unsubstituted pyridazines are more resistant to eletrophilic substitution due to the nature of withdrawal of electron density from the ring by two heteroatoms, while the related electron deficiency of the ring makes pyridazine more easily attacked by nucleophiles.Application In Synthesis of 3-Aminopyridazine

Referemce:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem

Synthesis of pyrido[2′,1′:2,3]imidazo[4,5-b]quinoline and pyrido[1′,2′:1,2]imidazo[4,5-b]quinoline and their benzo and aza analogs via tandem catalysis was written by Loones, Kristof T. J.;Maes, Bert U. W.;Dommisse, Roger A.. And the article was included in Tetrahedron in 2007.Recommanded Product: 5469-70-5 This article mentions the following:

Regioselective tandem metal-catalyzed aminations on 2-chloro-3-iodoquinoline and 2,3-dibromoquinoline with amino(benzo)(di)azines are reported. Eight new heterocyclic scaffolds of the dipyridoimidazole type could be synthesized. By controlling the reaction temperature selective C-2 intermol. Pd-catalyzed amination on 2,3-dibromoquinoline with amino(benzo)(di)azines can be achieved. In the experiment, the researchers used many compounds, for example, 3-Aminopyridazine (cas: 5469-70-5Recommanded Product: 5469-70-5).

3-Aminopyridazine (cas: 5469-70-5) belongs to pyridazine derivatives. The pyridazine structure is also found within the structure of several drugs such as cefozopran, cadralazine, minaprine, pipofezine, and hydralazine. Pyridazine is bioavailable (especially in the CNS) and can reduce toxicity. Pyridazine is a component of several drug molecules, and the pyridazine pharmacophore has contributed to a variety of pharmacologically active compounds.Recommanded Product: 5469-70-5

Referemce:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem

The discovery of a non-competitive GOT1 inhibitor, hydralazine hydrochloride, via a coupling reaction-based high-throughput screening assay was written by Wu, Qiqi;Sun, Zhongya;Chen, Zhifeng;Liu, Jingqiu;Ding, Hong;Luo, Cheng;Wang, Mingliang;Du, Daohai. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2022.Safety of 3-Aminopyridazine This article mentions the following:

Glutamate oxaloacetate transaminase 1 (GOT1) plays a key role in aberrant glutamine metabolism GOT1 suppression can arrest tumor growth and prevent the development of cancer, indicating GOT1 as a potential anticancer target. Reported GOT1 inhibitors, on the other hand, are quite restricted. Here, we developed and optimized a coupling reaction-based high-throughput screening assay for the discovery of GOT1 inhibitors. By using this screening assay, we found that the cardiovascular drug hydralazine hydrochloride inhibited GOT1 catalytic activity, with an IC50 of 26.62 ± 7.45 μM, in a non-competitive and partial-reversible manner. In addition, we determined the binding affinity of hydralazine hydrochloride to GOT1, with a Kd of 16.54 ± 8.59 μM, using a microscale thermophoresis assay. According to structure-activity relationship anal., the inhibitory activity of hydralazine hydrochloride is mainly derived from its hydrazine group. Furthermore, it inhibits the proliferation of cancer cells MCF-7 and MDA-MB-468 with a slight inhibitory effect compared to other tested cancer cells, highlighting GOT1 as a promising therapeutic target for the treatment of breast cancer. In the experiment, the researchers used many compounds, for example, 3-Aminopyridazine (cas: 5469-70-5Safety of 3-Aminopyridazine).

3-Aminopyridazine (cas: 5469-70-5) belongs to pyridazine derivatives. Pyridazine-based compounds continued to be a great source of biologically active compounds as evidenced by the number of publications which emerged in 2021. The activity depends upon the changes of substituted groups in the pyridazine ring system resulting in different biological activities. In addition, the natural pyrimidine bases uracil, thymine, and cytosine, which are constituents of the nucleic acids, are found to be the most important naturally occurring diazines.Safety of 3-Aminopyridazine

Referemce:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem