Category: 91912-53-7

The three-dimensional configuration of the ester heterocycle is basically the same as that of the carbocycle. Compound: 3-(Pyridin-4-yl)-1H-pyrazol-5-amine(SMILESS: NC1=CC(C2=CC=NC=C2)=NN1,cas:91912-53-7) is researched.Name: 5-Amino-2-fluoropyridine. The article 《Structure-activity relationship study, target identification, and pharmacological characterization of a small molecular IL-12/23 inhibitor, APY0201》 in relation to this compound, is published in Bioorganic & Medicinal Chemistry. Let’s take a look at the latest research on this compound (cas:91912-53-7).

Interleukin-12 (IL-12) and IL-23 are proinflammatory cytokines and therapeutic targets for inflammatory and autoimmune diseases, including inflammatory bowel diseases, psoriasis, rheumatoid arthritis, and multiple sclerosis. The authors describe the discovery of APY0201, a unique small mol. IL-12/23 production inhibitor, from activated macrophages and monocytes, and demonstrate ameliorated inflammation in an exptl. model of colitis. Through a chem. proteomics approach using a highly sensitive direct nanoflow LC-MS/MS system and bait compounds equipped with the FLAG epitope associated regulator of PIKfyve (ArPIKfyve) was detected. Further study identified its associated protein phosphoinositide kinase, FYVE finger-containing (PIKfyve), as the target protein of APY0201, which was characterized as a potent, highly selective, ATP-competitive PIKfyve inhibitor that interrupts the conversion of phosphatidylinositol 3-phosphate (PtdIns3P) to PtdIns(3,5)P2. These results elucidate the function of PIKfyve kinase in the IL-12/23 production pathway and in IL-12/23-driven inflammatory disease pathologies to provide a compelling rationale for targeting PIKfyve kinase in inflammatory and autoimmune diseases.

After consulting a lot of data, we found that this compound(91912-53-7)Related Products of 91912-53-7 can be used in many types of reactions. And in most cases, this compound has more advantages.

Reference:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

Quality Control of 3-(Pyridin-4-yl)-1H-pyrazol-5-amine. The reaction of aromatic heterocyclic molecules with protons is called protonation. Aromatic heterocycles are more basic than benzene due to the participation of heteroatoms. Compound: 3-(Pyridin-4-yl)-1H-pyrazol-5-amine, is researched, Molecular C8H8N4, CAS is 91912-53-7, about Synthesis and SAR studies of 5-(pyridin-4-yl)-1,3,4-thiadiazol-2-amine derivatives as potent inhibitors of Bloom helicase. Author is Rosenthal, Andrew S.; Dexheimer, Thomas S.; Gileadi, Opher; Nguyen, Giang H.; Chu, Wai Kit; Hickson, Ian D.; Jadhav, Ajit; Simeonov, Anton; Maloney, David J..

Human cells utilize a variety of complex DNA repair mechanisms to combat constant mutagenic and cytotoxic threats from both exogenous and endogenous sources. The RecQ family of DNA helicases, which includes Bloom helicase (BLM), plays an important function in DNA repair by unwinding complementary strands of duplex DNA and atypical DNA structures such as Holliday junctions. Mutations of the BLM gene can result in Bloom syndrome, an autosomal recessive disorder associated with cancer predisposition. BLM-deficient cells exhibit increased sensitivity to DNA damaging agents indicating that a selective BLM inhibitor could be useful in potentiating the anticancer activity of these agents. In this work, we describe the medicinal chem. optimization of the hit mol. following a quant. high-throughput screen of >355,000 compounds These efforts lead to the identification of ML216 and related analogs, which possess potent BLM inhibition and exhibit selectivity over related helicases. Moreover, these compounds demonstrated cellular activity by inducing sister chromatid exchanges, a hallmark of Bloom syndrome.

After consulting a lot of data, we found that this compound(91912-53-7)Quality Control of 3-(Pyridin-4-yl)-1H-pyrazol-5-amine can be used in many types of reactions. And in most cases, this compound has more advantages.

Reference:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

Electric Literature of C8H8N4. So far, in addition to halogen atoms, other non-metallic atoms can become part of the aromatic heterocycle, and the target ring system is still aromatic. Compound: 3-(Pyridin-4-yl)-1H-pyrazol-5-amine, is researched, Molecular C8H8N4, CAS is 91912-53-7, about Synthesis and study of the anti-inflammatory properties of some pyrazolo[1,5-a]pyrimidine derivatives.

A series of pyrazolo[1,5-a]pyrimidin-7-ones I (R = bromophenyl, methoxyphenyl, thienyl, pyridyl, cyclohexyl, Bu, iso-Pr, nitrophenyl, aminophenyl hydrochloride, and ethylpyridinium iodide) were synthesized to evaluate in vivo and in vitro effects induced by structural modifications at the 2 position of 4,7-dihydro-4-ethyl-2-phenylpyrazolo[1,5-a]pyrimidin-7-one (FPP028). This substance, which has been previously studied, is a weak inhibitor of prostaglandin biosynthesis and a nonacid analgesic and anti-inflammatory agent devoid of ulcerogenic properties. To gain more insight into the mechanism of action of this class of compounds, several in vivo tests were carried out, such as carrageenan-induced rat paw edema and pleurisy. In vitro tests include some studies of leukocyte functions, such as superoxide production and myeloperoxidase release. In vitro effects on arachidonic acid-, ADP, and platelet-activating factor-induced platelet aggregation were also studied. Different anti-inflammatory activities were observed, depending on the nature of substituents at the 2 position; these differences are probably linked to the capacity of these compounds to inhibit leukotrienes and/or prostaglandin biosynthesis with different selectivity. 4,7-Dihydro-4-ethyl-2(2-thienyl)pyrazolo[1,5-a]pyrimidin-7-one proved to be the most interesting compound of the novel synthesized series, showing powerful pharmacol. activity in vivo as well as in vitro, together with very weak acute toxicity.

After consulting a lot of data, we found that this compound(91912-53-7)Electric Literature of C8H8N4 can be used in many types of reactions. And in most cases, this compound has more advantages.

Reference:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

COA of Formula: C8H8N4. The reaction of aromatic heterocyclic molecules with protons is called protonation. Aromatic heterocycles are more basic than benzene due to the participation of heteroatoms. Compound: 3-(Pyridin-4-yl)-1H-pyrazol-5-amine, is researched, Molecular C8H8N4, CAS is 91912-53-7, about Synthesis and SAR studies of 5-(pyridin-4-yl)-1,3,4-thiadiazol-2-amine derivatives as potent inhibitors of Bloom helicase. Author is Rosenthal, Andrew S.; Dexheimer, Thomas S.; Gileadi, Opher; Nguyen, Giang H.; Chu, Wai Kit; Hickson, Ian D.; Jadhav, Ajit; Simeonov, Anton; Maloney, David J..

Human cells utilize a variety of complex DNA repair mechanisms to combat constant mutagenic and cytotoxic threats from both exogenous and endogenous sources. The RecQ family of DNA helicases, which includes Bloom helicase (BLM), plays an important function in DNA repair by unwinding complementary strands of duplex DNA and atypical DNA structures such as Holliday junctions. Mutations of the BLM gene can result in Bloom syndrome, an autosomal recessive disorder associated with cancer predisposition. BLM-deficient cells exhibit increased sensitivity to DNA damaging agents indicating that a selective BLM inhibitor could be useful in potentiating the anticancer activity of these agents. In this work, we describe the medicinal chem. optimization of the hit mol. following a quant. high-throughput screen of >355,000 compounds These efforts lead to the identification of ML216 and related analogs, which possess potent BLM inhibition and exhibit selectivity over related helicases. Moreover, these compounds demonstrated cellular activity by inducing sister chromatid exchanges, a hallmark of Bloom syndrome.

After consulting a lot of data, we found that this compound(91912-53-7)COA of Formula: C8H8N4 can be used in many types of reactions. And in most cases, this compound has more advantages.

Reference:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

Application of 91912-53-7. Aromatic heterocyclic compounds can also be classified according to the number of heteroatoms contained in the heterocycle: single heteroatom, two heteroatoms, three heteroatoms and four heteroatoms. Compound: 3-(Pyridin-4-yl)-1H-pyrazol-5-amine, is researched, Molecular C8H8N4, CAS is 91912-53-7, about Hit to lead optimization of pyrazolo[1,5-a]pyrimidines as B-Raf kinase inhibitors. Author is Gopalsamy, Ariamala; Ciszewski, Greg; Shi, Mengxiao; Berger, Dan; Hu, Yongbo; Lee, Frederick; Feldberg, Larry; Frommer, Eileen; Kim, Steven; Collins, Karen; Wojciechowicz, Donald; Mallon, Robert.

Our continued effort towards optimization of the pyrazolo[1,5-a]pyrimidine scaffold as B-Raf kinase inhibitors is described. Structure guided design was utilized to introduce kinase hinge region interacting groups in the 2-position of the scaffold. This strategy led to the identification of lead compound 9 with enhanced enzyme and cellular potency, while maintaining good selectivity over a number of kinases.

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Reference:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

In organic chemistry, atoms other than carbon and hydrogen are generally referred to as heteroatoms. The most common heteroatoms are nitrogen, oxygen and sulfur. Now I present to you an article called Design and Synthesis of the Potent, Orally Available, Brain-Penetrable Arylpyrazole Class of Neuropeptide Y5 Receptor Antagonists, published in 2003-02-27, which mentions a compound: 91912-53-7, mainly applied to indancarboxamide arylpyrazolyl preparation neuropeptide Y5 receptor antagonist, Formula: C8H8N4.

Novel arylpyrazole derivatives were synthesized and evaluated as neuropeptide Y5 receptor antagonists. The 2,3-dihydro-1H-cyclopenta[a]naphthalene derivative I showed good binding affinity and antagonistic activity for the Y5 receptor. After intracerebroventricular administration in SD rats, (-)-I significantly inhibited food intake that was induced by the centrally administered Y5-preferring agonist, bovine pancreatic polypeptide, but had only a negligible effect on NPY-induced feeding.

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Reference:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

Bruni, Fabrizio; Selleri, Silvia; Costanzo, Annarella; Guerrini, Gabriella; Ciciani, Giovanna; Costagli, Camilla; Sacco, Cristiana; Donato, Rosa published an article about the compound: 3-(Pyridin-4-yl)-1H-pyrazol-5-amine( cas:91912-53-7,SMILESS:NC1=CC(C2=CC=NC=C2)=NN1 ).Formula: C8H8N4. Aromatic heterocyclic compounds can be classified according to the number of heteroatoms or the size of the ring. The authors also want to convey more information about this compound (cas:91912-53-7) through the article.

A series of pyrazolo[1,5-a]pyrido[3,4-e]pyrimidin-6-ones, I (R1 = H, Me, Ph, 2-furyl, etc., R2 = cyano, CO2Et, H, Ph, NO2, Cl, R3, R4 = H, Me), was prepared by a simple synthetic procedure based on the reaction of hydroxylamine or methoxyamine with 2,3-substituted Et 7-dimethylaminovinyl pyrazolo[1,5-a]pyrimidin-6-carboxylates II. The antimicrobial activity of the obtained compounds was evaluated on a series of standard strains of Gram pos., Gram neg. bacteria and fungi. None of the tested compounds showed significant activity.

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Reference:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

Gopalsamy, Ariamala; Ciszewski, Greg; Shi, Mengxiao; Berger, Dan; Hu, Yongbo; Lee, Frederick; Feldberg, Larry; Frommer, Eileen; Kim, Steven; Collins, Karen; Wojciechowicz, Donald; Mallon, Robert published an article about the compound: 3-(Pyridin-4-yl)-1H-pyrazol-5-amine( cas:91912-53-7,SMILESS:NC1=CC(C2=CC=NC=C2)=NN1 ).Category: pyrazines. Aromatic heterocyclic compounds can be classified according to the number of heteroatoms or the size of the ring. The authors also want to convey more information about this compound (cas:91912-53-7) through the article.

Our continued effort towards optimization of the pyrazolo[1,5-a]pyrimidine scaffold as B-Raf kinase inhibitors is described. Structure guided design was utilized to introduce kinase hinge region interacting groups in the 2-position of the scaffold. This strategy led to the identification of lead compound 9 with enhanced enzyme and cellular potency, while maintaining good selectivity over a number of kinases.

Compounds in my other articles are similar to this one(3-(Pyridin-4-yl)-1H-pyrazol-5-amine)Category: pyrazines, you can compare them to see their pros and cons in some ways,such as convenient, effective and so on.

Reference:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

Synthetic Route of C8H8N4. Aromatic compounds can be divided into two categories: single heterocycles and fused heterocycles. Compound: 3-(Pyridin-4-yl)-1H-pyrazol-5-amine, is researched, Molecular C8H8N4, CAS is 91912-53-7, about Hit to lead optimization of pyrazolo[1,5-a]pyrimidines as B-Raf kinase inhibitors. Author is Gopalsamy, Ariamala; Ciszewski, Greg; Shi, Mengxiao; Berger, Dan; Hu, Yongbo; Lee, Frederick; Feldberg, Larry; Frommer, Eileen; Kim, Steven; Collins, Karen; Wojciechowicz, Donald; Mallon, Robert.

Our continued effort towards optimization of the pyrazolo[1,5-a]pyrimidine scaffold as B-Raf kinase inhibitors is described. Structure guided design was utilized to introduce kinase hinge region interacting groups in the 2-position of the scaffold. This strategy led to the identification of lead compound 9 with enhanced enzyme and cellular potency, while maintaining good selectivity over a number of kinases.

In some applications, this compound(91912-53-7)Synthetic Route of C8H8N4 is unique.If you want to know more details about this compound, you can contact with the author or consult more relevant literature.

Reference:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

Related Products of 91912-53-7. Aromatic compounds can be divided into two categories: single heterocycles and fused heterocycles. Compound: 3-(Pyridin-4-yl)-1H-pyrazol-5-amine, is researched, Molecular C8H8N4, CAS is 91912-53-7, about Design and Synthesis of the Potent, Orally Available, Brain-Penetrable Arylpyrazole Class of Neuropeptide Y5 Receptor Antagonists. Author is Sato, Nagaaki; Takahashi, Toshiyuki; Shibata, Takunobu; Haga, Yuji; Sakuraba, Aya; Hirose, Masaaki; Sato, Miki; Nonoshita, Katsumasa; Koike, Yuko; Kitazawa, Hidefumi; Fujino, Naoko; Ishii, Yasuyuki; Ishihara, Akane; Kanatani, Akio; Fukami, Takehiro.

Novel arylpyrazole derivatives were synthesized and evaluated as neuropeptide Y5 receptor antagonists. The 2,3-dihydro-1H-cyclopenta[a]naphthalene derivative I showed good binding affinity and antagonistic activity for the Y5 receptor. After intracerebroventricular administration in SD rats, (-)-I significantly inhibited food intake that was induced by the centrally administered Y5-preferring agonist, bovine pancreatic polypeptide, but had only a negligible effect on NPY-induced feeding.

As far as I know, this compound(91912-53-7)Related Products of 91912-53-7 can be applied in many ways, which is helpful for the development of experiments. Therefore many people are doing relevant researches.

Reference:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem