Yuan, Xinrui’s team published research in Bioorganic & Medicinal Chemistry in 2019-04-01 | 20744-39-2

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.

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

 

Kappe, T.’s team published research in Synthesis in 1989 | CAS: 40020-05-1

4,6-Dichloro-3-phenylpyridazine(cas: 40020-05-1) belongs to pyridazine. The pyridazine moiety is an important structural feature of various pharmacologically important compounds with activities like antimicrobial, neuroleptic, sedative-hypnotic, analgesic, anti-inflammatory, antiplatelet, anticancer, antisecretory, antiulcer, antidepressant, anticonvulsant, immunosuppressant, cardiotonic, vasodilator, antiarrhythmic, and hypocholesterolaemic. Synthetic Route of C10H6Cl2N2

Synthetic Route of C10H6Cl2N2On September 30, 1989 ,《Organic azides in heterocyclic synthesis. 8. Synthesis of aminopyridazines from Azidopyridazines and tetrazolo[1,5-b]pyridazines》 was published in Synthesis. The article was written by Kappe, T.; Pfaffenschlager, A.; Stadlbauer, W.. The article contains the following contents:

Azidopyridazines and tetrazolo[1,5-b]pyridazines can be converted to the corresponding aminopyridazines, by reaction with triphenylphosphine via phosphazenes and subsequent hydrolysis (Staudinger reaction). In addition to this study using 4,6-Dichloro-3-phenylpyridazine, there are many other studies that have used 4,6-Dichloro-3-phenylpyridazine(cas: 40020-05-1Synthetic Route of C10H6Cl2N2) was used in this study.

4,6-Dichloro-3-phenylpyridazine(cas: 40020-05-1) belongs to pyridazine. The pyridazine moiety is an important structural feature of various pharmacologically important compounds with activities like antimicrobial, neuroleptic, sedative-hypnotic, analgesic, anti-inflammatory, antiplatelet, anticancer, antisecretory, antiulcer, antidepressant, anticonvulsant, immunosuppressant, cardiotonic, vasodilator, antiarrhythmic, and hypocholesterolaemic. Synthetic Route of C10H6Cl2N2

Referemce:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem

 

Stadlbauer, W.’s team published research in Synthesis in 1989 | CAS: 40020-05-1

4,6-Dichloro-3-phenylpyridazine(cas: 40020-05-1) belongs to pyridazine. The pyridazine moiety is an important structural feature of various pharmacologically important compounds with activities like antimicrobial, antiplatelet, anticancer, antisecretory, analgesic, anti-inflammatory, antiulcer, antidepressant, neuroleptic, sedative-hypnotic, anticonvulsant, immunosuppressant, cardiotonic, vasodilator, antiarrhythmic, and hypocholesterolaemic. HPLC of Formula: 40020-05-1

HPLC of Formula: 40020-05-1On October 31, 1989 ,《Organic azides in heterocyclic synthesis. Part 9. Ring closure of 4-azido-3-phenylpyridazines to pyridazino[4,3-b]indoles》 was published in Synthesis. The article was written by Stadlbauer, W.; Pfaffenschlager, A.; Kappe, T.. The article contains the following contents:

The cyclization of 4-azido-3-phenylpyridazines I (R = Cl, OH) and 7-azido-6-phenyltetrazolo[1,5-b]pyridazine II by heating with strong acids like MeSO3H affords 5H-pyridazino[4,3-b]indoles III or 10H-tetrazolo[1′,5′:1,6]pyridazino[4,3-b]indole IV, resp., whereas conventional photochem. and thermolytic methods fail. In the experiment, the researchers used many compounds, for example, 4,6-Dichloro-3-phenylpyridazine(cas: 40020-05-1HPLC of Formula: 40020-05-1)

4,6-Dichloro-3-phenylpyridazine(cas: 40020-05-1) belongs to pyridazine. The pyridazine moiety is an important structural feature of various pharmacologically important compounds with activities like antimicrobial, antiplatelet, anticancer, antisecretory, analgesic, anti-inflammatory, antiulcer, antidepressant, neuroleptic, sedative-hypnotic, anticonvulsant, immunosuppressant, cardiotonic, vasodilator, antiarrhythmic, and hypocholesterolaemic. HPLC of Formula: 40020-05-1

Referemce:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem

 

Haider, N.’s team published research in Science of Synthesis in 2004 | CAS: 62567-44-6

3-Ethoxypyridazine(cas: 62567-44-6) belongs to pyridazine derivatives.The pyridazine derivatives are mostly present in biologically active compounds and are also present with different pharmacophores. Pyridazines are also important because of their utility in synthetic organic chemistry and in physical organic chemistry.There are reports available for the synthesis of pyridazine and their derivatives by using 2-oxoaldehyes.Category: pyridazine

《Product class 8: pyridazines》 was published in Science of Synthesis in 2004. These research results belong to Haider, N.; Holzer, W.. Category: pyridazine The article mentions the following:

A review. Methods of preparing pyridazines are reviewed including cyclization, ring transformation, aromatization, and substituent modification. The experimental process involved the reaction of 3-Ethoxypyridazine(cas: 62567-44-6Category: pyridazine)

3-Ethoxypyridazine(cas: 62567-44-6) belongs to pyridazine derivatives.The pyridazine derivatives are mostly present in biologically active compounds and are also present with different pharmacophores. Pyridazines are also important because of their utility in synthetic organic chemistry and in physical organic chemistry.There are reports available for the synthesis of pyridazine and their derivatives by using 2-oxoaldehyes.Category: pyridazine

Referemce:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem

 

Donohoe, Timothy J.’s team published research in Tetrahedron in 2009 | CAS: 62567-44-6

3-Ethoxypyridazine(cas: 62567-44-6) belongs to pyridazine derivatives.The pyridazine derivatives are mostly present in biologically active compounds and are also present with different pharmacophores. Pyridazines are also important because of their utility in synthetic organic chemistry and in physical organic chemistry.There are reports available for the synthesis of pyridazine and their derivatives by using 2-oxoaldehyes.Application of 62567-44-6

Application of 62567-44-6On October 31, 2009 ,《Ring-closing metathesis for the synthesis of heteroaromatics: evaluating routes to pyridines and pyridazines》 appeared in Tetrahedron. The author of the article were Donohoe, Timothy J.; Bower, John F.; Basutto, Jose A.; Fishlock, Lisa P.; Procopiou, Panayiotis A.; Callens, Cedric K. A.. The article conveys some information:

Ring-closing olefin metathesis (RCM) has been applied to the efficient synthesis of densely and diversely substituted pyridine and pyridazine frameworks. Routes to suitable metathesis precursors have been investigated and the scope of the metathesis step has been probed. The metathesis products function as precursors to the target heteroaromatic structures via elimination of a suitable leaving group, which also facilitates earlier steps by serving as a protecting group at nitrogen. Further functionalization of the metathesis products is possible both prior to and after aromatization. The net result is a powerful strategy for the de novo synthesis of highly substituted heteroaromatic scaffolds. In the experiment, the researchers used 3-Ethoxypyridazine(cas: 62567-44-6Application of 62567-44-6)

3-Ethoxypyridazine(cas: 62567-44-6) belongs to pyridazine derivatives.The pyridazine derivatives are mostly present in biologically active compounds and are also present with different pharmacophores. Pyridazines are also important because of their utility in synthetic organic chemistry and in physical organic chemistry.There are reports available for the synthesis of pyridazine and their derivatives by using 2-oxoaldehyes.Application of 62567-44-6

Referemce:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem

 

Blagoeva, I.’s team published research in Izvestiya po Khimiya in 1988 | CAS: 40020-05-1

4,6-Dichloro-3-phenylpyridazine(cas: 40020-05-1) belongs to pyridazine. The pyridazine moiety is an important structural feature of various pharmacologically important compounds with activities like antimicrobial, sedative-hypnotic, anticonvulsant, analgesic, anti-inflammatory, antiplatelet, anticancer, antisecretory, antiulcer, antidepressant, neuroleptic, immunosuppressant, cardiotonic, vasodilator, antiarrhythmic, and hypocholesterolaemic. Safety of 4,6-Dichloro-3-phenylpyridazine

《Effect of a neighboring methyl group on the acid- and base-catalyzed cyclizations of 2-ureidobenzoic acids》 was published in Izvestiya po Khimiya in 1988. These research results belong to Blagoeva, I.; Koedzhikov, A.; Pozharliev, I.. Safety of 4,6-Dichloro-3-phenylpyridazine The article mentions the following:

The cyclization of title compound I (R = H) in acid is 1.6 times slower than that of I (R = Me); in base, however, I (R = H) cyclizes 16 times faster than I (R = Me). The rates are interpreted in terms of resonance stabilization of CO2H but not CO2- and steric hindrance in the transition state. In the base-catalyzed process, a change in rate-determining step occurs as the alkalinity is increased. In the experiment, the researchers used 4,6-Dichloro-3-phenylpyridazine(cas: 40020-05-1Safety of 4,6-Dichloro-3-phenylpyridazine)

4,6-Dichloro-3-phenylpyridazine(cas: 40020-05-1) belongs to pyridazine. The pyridazine moiety is an important structural feature of various pharmacologically important compounds with activities like antimicrobial, sedative-hypnotic, anticonvulsant, analgesic, anti-inflammatory, antiplatelet, anticancer, antisecretory, antiulcer, antidepressant, neuroleptic, immunosuppressant, cardiotonic, vasodilator, antiarrhythmic, and hypocholesterolaemic. Safety of 4,6-Dichloro-3-phenylpyridazine

Referemce:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem

 

Landvoigt, Werner’s team published research in Mikrochimica Acta in 1982 | CAS: 40020-05-1

4,6-Dichloro-3-phenylpyridazine(cas: 40020-05-1) belongs to pyridazine. The pyridazine moiety is an important structural feature of various pharmacologically important compounds with activities like antimicrobial, cardiotonic, vasodilator, analgesic, anti-inflammatory, antiplatelet, anticancer, antisecretory, antiulcer, antidepressant, neuroleptic, sedative-hypnotic, anticonvulsant, immunosuppressant, antiarrhythmic, and hypocholesterolaemic. Recommanded Product: 4,6-Dichloro-3-phenylpyridazine

《Formation of a 3-phenyl-4-hydroxy-6-chloropyridazine derivative for GC with ECD and MS detection and its application to trace analysis》 was published in Mikrochimica Acta in 1982. These research results belong to Landvoigt, Werner; Malissa, Hans Jr.; Winsauer, Karl. Recommanded Product: 4,6-Dichloro-3-phenylpyridazine The article mentions the following:

The determination of Pyridate (I) [55512-33-9] and the metabolite CL 9673 (II, 6-chloro-4-hydroxy-3-phenylpyridazine) [40020-01-7] is described. The method permits the determination of both compounds sep. and is applicable to corn and rape crops. The reaction of pentafluorobenzoyl chloride  [2251-50-5] with II, important in the assay, is described. The product 6-chloro-4-pentafluorobenzoyl-3-phenylpyridazine  [83607-25-4] is unstable; when the reaction is run in dioxan or THF solvent, 4,6-dichloro-3-phenylpyridazine  [40020-05-1], a stable compound, is formed. This chloro derivative is easily determined by TLC, with detection limits of ∼1 μg/mL. Trace amounts are determined by an alternate method wherein, following separation of I and II by chromatog., II is brominated with POBr3, and determined by capillary gas chromatog. coupled with mass spectrometry. I is determined by saponification to II, and then determined as the brominated derivative as described. Detection limits are 10 ng/g.4,6-Dichloro-3-phenylpyridazine(cas: 40020-05-1Recommanded Product: 4,6-Dichloro-3-phenylpyridazine) was used in this study.

4,6-Dichloro-3-phenylpyridazine(cas: 40020-05-1) belongs to pyridazine. The pyridazine moiety is an important structural feature of various pharmacologically important compounds with activities like antimicrobial, cardiotonic, vasodilator, analgesic, anti-inflammatory, antiplatelet, anticancer, antisecretory, antiulcer, antidepressant, neuroleptic, sedative-hypnotic, anticonvulsant, immunosuppressant, antiarrhythmic, and hypocholesterolaemic. Recommanded Product: 4,6-Dichloro-3-phenylpyridazine

Referemce:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem

 

Czech, Karin’s team published research in Monatshefte fuer Chemie in 1991 | CAS: 1445-56-3

3-Chloropyridazine-4-carbonitrile(cas: 1445-56-3) belongs to pyridazine derivatives.The pyridazine derivatives are mostly present in biologically active compounds and are also present with different pharmacophores. Pyridazines are also important because of their utility in synthetic organic chemistry and in physical organic chemistry.There are reports available for the synthesis of pyridazine and their derivatives by using 2-oxoaldehyes.Safety of 3-Chloropyridazine-4-carbonitrile

Safety of 3-Chloropyridazine-4-carbonitrileOn May 31, 1991, Czech, Karin; Haider, Norbert; Heinisch, Gottfried published an article in Monatshefte fuer Chemie. The article was 《Pyridazines. LIV. The synthesis of pyridazine-fused S-heterocycles: thieno[2,3-c]pyridazine, pyrimido[4′,5′:4,5]thieno[2,3-c]pyridazine, and pyridazino[3,4-b][1,4]benzothiazine》. The article mentions the following:

Starting from 3-chloro-4-pyridazinecarbonitrile (I), the thienopyridazine derivatives II (R = OMe; R1 = OMe, NH2) were prepared Condensation of II (R = NH2) with (EtO3)CH afforded the novel tricyclic system III. Reaction of I (R = R1 = NH2) with 2-H2NC6H4SH, followed by treatment with NaH/DMSO gave pyridazinobenzothiazine IV instead of the expected condensed thiazepine. In the experiment, the researchers used many compounds, for example, 3-Chloropyridazine-4-carbonitrile(cas: 1445-56-3Safety of 3-Chloropyridazine-4-carbonitrile)

3-Chloropyridazine-4-carbonitrile(cas: 1445-56-3) belongs to pyridazine derivatives.The pyridazine derivatives are mostly present in biologically active compounds and are also present with different pharmacophores. Pyridazines are also important because of their utility in synthetic organic chemistry and in physical organic chemistry.There are reports available for the synthesis of pyridazine and their derivatives by using 2-oxoaldehyes.Safety of 3-Chloropyridazine-4-carbonitrile

Referemce:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem

 

Dostal, Wolfgang’s team published research in Monatshefte fuer Chemie in 1988 | CAS: 1445-56-3

3-Chloropyridazine-4-carbonitrile(cas: 1445-56-3) belongs to pyridazine derivatives.The pyridazine derivatives are mostly present in biologically active compounds and are also present with different pharmacophores. Pyridazines are also important because of their utility in synthetic organic chemistry and in physical organic chemistry.There are reports available for the synthesis of pyridazine and their derivatives by using 2-oxoaldehyes.Name: 3-Chloropyridazine-4-carbonitrile

Dostal, Wolfgang; Heinisch, Gottfried; Loetsch, Gerhard published an article in Monatshefte fuer Chemie. The title of the article was 《Chemistry of pyridazines. XXXVI. Novel diaza-analogs of 10,11-dihydro-5H-dibenzo[a,d]cyclohepten-5-one》.Name: 3-Chloropyridazine-4-carbonitrile The author mentioned the following in the article:

Procedures for the preparation of the novel tricyclic ketones 10,11-dihydro-5H-benzo[4,5]cyclohepta[1,2-d]pyridazin-5-one (I), 5,6-dihydro-11H-benzo[4,5]cyclohepta[2,1-c]pyridazin-11-one, and 10,11-dihydro-5H-benzo[4,5]cyclohepta[1,2-c]pyridazin-5-one starting from a preformed 1,2-diazine system are proposed. The key intermediates, e.g., II (R = CO2Et) are prepared from (2-phenylethyl)pyridazines, e.g., II (R = H) by introduction of a carboxylic functionality via homolytic alkoxycarbonylation or via a sulfonyl Reissert-type reaction. The experimental process involved the reaction of 3-Chloropyridazine-4-carbonitrile(cas: 1445-56-3Name: 3-Chloropyridazine-4-carbonitrile)

3-Chloropyridazine-4-carbonitrile(cas: 1445-56-3) belongs to pyridazine derivatives.The pyridazine derivatives are mostly present in biologically active compounds and are also present with different pharmacophores. Pyridazines are also important because of their utility in synthetic organic chemistry and in physical organic chemistry.There are reports available for the synthesis of pyridazine and their derivatives by using 2-oxoaldehyes.Name: 3-Chloropyridazine-4-carbonitrile

Referemce:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem

 

Munoz, Lenka’s team published research in Journal of Neuroinflammation in 2007 | CAS: 40020-05-1

4,6-Dichloro-3-phenylpyridazine(cas: 40020-05-1) belongs to pyridazine. The pyridazine moiety is an important structural feature of various pharmacologically important compounds with activities like antimicrobial, antiulcer, antidepressant, neuroleptic, sedative-hypnotic, anticonvulsant, analgesic, anti-inflammatory, antiplatelet, anticancer, antisecretory, immunosuppressant, cardiotonic, vasodilator, antiarrhythmic, and hypocholesterolaemic. Quality Control of 4,6-Dichloro-3-phenylpyridazine

《A novel p38α MAPK inhibitor suppresses brain proinflammatory cytokine up-regulation and attenuates synaptic dysfunction and behavioral deficits in an Alzheimer’s disease mouse model》 was published in Journal of Neuroinflammation in 2007. These research results belong to Munoz, Lenka; Ranaivo, Hantamalala Ralay; Roy, Saktimayee M.; Hu, Wenhui; Craft, Jeffrey M.; McNamara, Laurie K.; Chico, Laura Wing; Van Eldik, Linda J.; Watterson, D. Martin. Quality Control of 4,6-Dichloro-3-phenylpyridazine The article mentions the following:

Background: An accumulating body of evidence is consistent with the hypothesis that excessive or prolonged increases in proinflammatory cytokine production by activated glia is a contributor to the progression of pathophysiol. that is causally linked to synaptic dysfunction and hippocampal behavior deficits in neurodegenerative diseases such as Alzheimer’s disease (AD). This raises the opportunity for the development of new classes of potentially disease-modifying therapeutics. A logical candidate CNS target is p38α MAPK, a well-established drug discovery mol. target for altering proinflammatory cytokine cascades in peripheral tissue disorders. Activated p38 MAPK is seen in human AD brain tissue and in AD-relevant animal models, and cell culture studies strongly implicate p38 MAPK in the increased production of proinflammatory cytokines by glia activated with human amyloid-beta (Aβ) and other disease-relevant stressors. However, the vast majority of small mol. drugs do not have sufficient penetrance of the blood-brain barrier to allow their use as in vivo research tools or as therapeutics for neurodegenerative disorders. The goal of this study was to test the hypothesis that brain p38α MAPK is a potential in vivo target for orally bioavailable, small mols. capable of suppressing excessive cytokine production by activated glia back towards homeostasis, allowing an improvement in neurol. outcomes. Methods: A novel synthetic small mol. based on a mol. scaffold used previously was designed, synthesized, and subjected to analyses to demonstrate its potential in vivo bioavailability, metabolic stability, safety and brain uptake. Testing for in vivo efficacy used an AD-relevant mouse model. Results: A novel, CNS-penetrant, non-toxic, orally bioavailable, small mol. inhibitor of p38α MAPK (MW01-2-069A-SRM) was developed. Oral administration of the compound at a low dose (2.5 mg/kg) resulted in attenuation of excessive proinflammatory cytokine production in the hippocampus back towards normal in the animal model. Animals with attenuated cytokine production had reductions in synaptic dysfunction and hippocampus-dependent behavioral deficits. Conclusion: The p38α MAPK pathway is quant. important in the Aβ-induced production of proinflammatory cytokines in hippocampus, and brain p38α MAPK is a viable mol. target for future development of potential disease-modifying therapeutics in AD and related neurodegenerative disorders.4,6-Dichloro-3-phenylpyridazine(cas: 40020-05-1Quality Control of 4,6-Dichloro-3-phenylpyridazine) was used in this study.

4,6-Dichloro-3-phenylpyridazine(cas: 40020-05-1) belongs to pyridazine. The pyridazine moiety is an important structural feature of various pharmacologically important compounds with activities like antimicrobial, antiulcer, antidepressant, neuroleptic, sedative-hypnotic, anticonvulsant, analgesic, anti-inflammatory, antiplatelet, anticancer, antisecretory, immunosuppressant, cardiotonic, vasodilator, antiarrhythmic, and hypocholesterolaemic. Quality Control of 4,6-Dichloro-3-phenylpyridazine

Referemce:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem