Tag: 200-300

《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

《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

《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

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

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

Olesen, Preben H.; Kappe, Thomas; Becher, jan published their research in Journal of Heterocyclic Chemistry on December 31 ,1988. The article was titled 《Pyridazines with heteroatom substituents in position 3 and 5. 2. Regioselective introduction of mercapto groups in pyridazines》.Application In Synthesis of 4,6-Dichloro-3-phenylpyridazine The article contains the following contents:

The nucleophilic substitution of halogen in 3,5-dichloro-6-phenylpyridazine (I), 5-chloro-2-methyl-6-phenylpyridazin-3(2H)-one (II, R = Cl, R1 = Me, X = O) and 3-chloro-2-methyl-6-phenylpyridazin-5(2H)-one (III, R = Cl, R1 = Me) with MeONa, EtONa, and Me3CSNa is described. In the last type of compounds, the Me3CS groups can be eliminated regioselectively with Lewis acids, resulting in the formation of monomercapto and monothiopyridazines II (R = SH, R1 = H, Me, X = O, S) and III (R = SH, R1 = H, Me). After reading the article, we found that the author used 4,6-Dichloro-3-phenylpyridazine(cas: 40020-05-1Application In Synthesis 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, analgesic, anti-inflammatory, antiplatelet, anticancer, antisecretory, antiulcer, antidepressant, neuroleptic, sedative-hypnotic, anticonvulsant, immunosuppressant, cardiotonic, vasodilator, antiarrhythmic, and hypocholesterolaemic. Application In Synthesis of 4,6-Dichloro-3-phenylpyridazine

Referemce:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem

《Synthesis, reactions, and spectroscopy of 3-benzoyl-6-phenylpyridazines of expected biological activity》 was written by Issac, Yvette A.. Recommanded Product: 40020-05-1 And the article was included in Zeitschrift fuer Naturforschung, B: Chemical Sciences on August 31 ,1999. The article conveys some information:

Oxidative decyanation of α,6-diphenyl-3-pyridazineacetonitrile in MeOH yielded 3-benzoyl-6-phenylpyridazine (I). α,6-Diphenyl-3-pyridazinemethanol was obtained via NaBH4 reduction of I. Reaction of I with NH2OH or its O-alkyl derivatives yields 3-benzoyl-6-phenylpyridazine oxime (II) and alkyloximes, resp. Treatment of II with AcOH/H2SO4 afforded I again and not the rearranged products. Beckmann rearrangement was achieved for II and the corresponding ethyloxime giving solely 3-carboxanilide-6-phenylpyridazine. 4-Benzoyl-3-phenyl-6-chloropyridazine oxime was synthesized from the corresponding ketone. The results came from multiple reactions, including the reaction of 4,6-Dichloro-3-phenylpyridazine(cas: 40020-05-1Recommanded Product: 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, vasodilator, antiarrhythmic, analgesic, anti-inflammatory, antiplatelet, anticancer, antisecretory, antiulcer, antidepressant, neuroleptic, sedative-hypnotic, anticonvulsant, immunosuppressant, cardiotonic, and hypocholesterolaemic. Recommanded Product: 40020-05-1

Referemce:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem

Synthetic Route of C6H5BrN2O2In 2021, Heinrich, Timo;Sala-Hojman, Ada;Ferretti, Roberta;Petersson, Carl;Minguzzi, Stefano;Gondela, Andrzej;Ramaswamy, Shivapriya;Bartosik, Anna;Czauderna, Frank;Crowley, Lindsey;Wahra, Pamela;Schilke, Heike;Boepple, Pia;Dudek, Lukasz;Les, Marcin;Niedziejko, Paulina;Olech, Kamila;Pawlik, Henryk;Wloszczak, Lukasz;Zuchowicz, Karol;Suarez Alvarez, Jose Ramon;Martyka, Justyna;Sitek, Ewa;Mikulski, Maciej;Szczesniak, Joanna;Jaeckel, Sven;Krier, Mireille;Krol, Marcin;Wegener, Ansgar;Galezowski, Michal;Nowak, Mateusz;Becker, Frank;Herhaus, Christian published 《Discovery of 5-{2-[5-Chloro-2-(5-ethoxyquinoline-8-sulfonamido)phenyl]ethynyl}-4-methoxypyridine-2-carboxylic Acid, a Highly Selective in Vivo Useable Chemical Probe to Dissect MCT4 Biology》. 《Journal of Medicinal Chemistry》published the findings. The article contains the following contents:

Due to increased lactate production during glucose metabolism, tumor cells heavily rely on efficient lactate transport to avoid intracellular lactate accumulation and acidification. Monocarboxylate transporter 4 (MCT4/SLC16A3) is a lactate transporter that plays a central role in tumor pH modulation. The discovery and optimization of a novel class of MCT4 inhibitors (hit 9a), identified by a cellular screening in MDA-MB-231, is described. Direct target interaction of the optimized compound 18n with the cytosolic domain of MCT4 was shown after solubilization of the GFP-tagged transporter by fluorescence cross-correlation spectroscopy and microscopic studies. In vitro treatment with 18n resulted in lactate efflux inhibition and reduction of cellular viability in MCT4 high expressing cells. Moreover, pharmacokinetic properties of 18n allowed assessment of lactate modulation and antitumor activity in a mouse tumor model. Thus, 18n represents a valuable tool for investigating selective MCT4 inhibition and its effect on tumor biol. And Methyl 6-bromopyridazine-3-carboxylate (cas: 65202-52-0) was used in the research process.

The pyridazine structure is a popular pharmacophore which is found within a number of herbicides such as credazine, pyridafol and pyridate.Synthetic Route of C6H5BrN2O2 It is also found within the structure of several drugs such as cefozopran, cadralazine, minaprine, pipofezine, and hydralazine.

Reference:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem

Related Products of 65202-52-0《Structure-activity relationship study of 4-(thiazol-5-yl)benzoic acid derivatives as potent protein kinase CK2 inhibitors》 was published in 2016. The authors were Ohno, Hiroaki;Minamiguchi, Daiki;Nakamura, Shinya;Shu, Keito;Okazaki, Shiho;Honda, Maho;Misu, Ryosuke;Moriwaki, Hirotomo;Nakanishi, Shinsuke;Oishi, Shinya;Kinoshita, Takayoshi;Nakanishi, Isao;Fujii, Nobutaka, and the article was included in《Bioorganic & Medicinal Chemistry》. The author mentioned the following in the article:

Two classes of modified analogs of 4-(thiazol-5-yl)benzoic acid-type CK2 inhibitors were designed. The azabenzene analogs, pyridine- and pyridazine-carboxylic acid derivatives, showed potent protein kinase CK2 inhibitory activities [IC₅₀ (CK2α) = 0.014-0.017 μM; IC₅₀ (CK2α’) = 0.0046-0.010 μM]. Introduction of a 2-halo- or 2-methoxy-benzyloxy group at the 3-position of the benzoic acid moiety maintained the potent CK2 inhibitory activities [IC₅₀ (CK2α) = 0.014-0.016 μM; IC₅₀ (CK2α’) = 0.0088-0.014 μM] and led to antiproliferative activities [CC₅₀ (A549) = 1.5-3.3 μM] three to six times higher than those of the parent compound To complete the study, the researchers used Methyl 6-bromopyridazine-3-carboxylate (cas: 65202-52-0) .

The pyridazine structure is a popular pharmacophore which is found within a number of herbicides such as credazine, pyridafol and pyridate.Related Products of 65202-52-0 It is also found within the structure of several drugs such as cefozopran, cadralazine, minaprine, pipofezine, and hydralazine.

Reference:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem

Barlin, Gordon B.;Yap, C. Yoot published 《Some 3-halopyridazines》. The research results were published in《Australian Journal of Chemistry》 in 1977.COA of Formula: C6H5BrN2O2 The article conveys some information:

3-Halogenopyridazines including 3-fluoro-6-methyl- and 3-iodo-pyridazines; Me 3-fluoro-, 3-bromo- and 3-iodopyridazine-6-carboxylates and some intermediates were prepared Thus, Me 3-hydroxypyridazine-6-carboxylate was treated with POCl₃ to give Me 3-chloropyridazine-6-carboxylate. To complete the study, the researchers used Methyl 6-bromopyridazine-3-carboxylate (cas: 65202-52-0) .

The pyridazine structure is a popular pharmacophore which is found within a number of herbicides such as credazine, pyridafol and pyridate.COA of Formula: C6H5BrN2O2 It is also found within the structure of several drugs such as cefozopran, cadralazine, minaprine, pipofezine, and hydralazine.

Reference:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem