Category: 91912-53-7

Heterocyclic compounds can be divided into two categories: alicyclic heterocycles and aromatic heterocycles. Compounds whose heterocycles in the molecular skeleton cannot reflect aromaticity are called alicyclic heterocyclic compounds. Compound: 91912-53-7, is researched, Molecular C8H8N4, about Pyrazolo[1,5-a]pyrido[3,4-e]pyrimidin-6-ones. II. Synthesis and in vitro antimicrobial evaluation, the main research direction is pyrazolopyridopyrimidinone preparation bactericide fungicide; pyridopyrimidinone pyrazolo preparation bactericide fungicide; pyrimidinone pyrazolopyrido preparation bactericide fungicide.Product Details of 91912-53-7.

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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Most of the compounds have physiologically active properties, and their biological properties are often attributed to the heteroatoms contained in their molecules, and most of these heteroatoms also appear in cyclic structures. A Journal, Article, Journal of Medicinal Chemistry called 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, which mentions a compound: 91912-53-7, SMILESS is NC1=CC(C2=CC=NC=C2)=NN1, Molecular C8H8N4, COA of 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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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 Novel pyrazolopyrimidines as highly potent B-Raf inhibitors, published in 2009-12-15, which mentions a compound: 91912-53-7, mainly applied to cancer B Raf inhibitor indazole pyrazolopyrimidine derivative SAR preparation, Recommanded Product: 91912-53-7.

A novel series of pyrazolo[1,5-a]pyrimidines bearing a 3-hydroxyphenyl group at C(3) and substituted tropanes at C(7) have been identified as potent B-Raf inhibitors. Exploration of alternative functional groups as a replacement for the C(3) phenol demonstrated indazole to be an effective isostere. Several compounds possessing substituted indazole residues, such as 4e, 4p, and 4r, potently inhibited cell proliferation at submicromolar concentrations in the A375 and WM266 cell lines, and the latter two compounds also exhibited good therapeutic indexes in cells.

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The chemical properties of alicyclic heterocycles are similar to those of the corresponding chain compounds. 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, the main research direction is pyridinylthiadiazolamine derivative preparation SAR Bloom helicase inhibitor; ADME; BLM; BS; Bloom helicase; Bloom syndrome; DMF; HR; HTS; Inhibitor; MLM; NADPH; PBS; PEPPSITM-IPr; SAR; SCE; Small molecule; [1,3-Bis(2,6-Diisopropylphenyl)imidazole-2-ylidene](3-chloropyridyl)palladium(II)chloride; absorption, distribution, metabolism and excretion; dimethylformamide; high throughput screen; homologous recombination; mouse liver microsomes; nicotinamide adenine dinucleotide phosphate; phosphate buffered saline; sister chromatid exchanges; structure activity relationship.Application In Synthesis of 3-(Pyridin-4-yl)-1H-pyrazol-5-amine.

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.

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The reaction of an aromatic heterocycle with a proton is called a protonation. One of articles about this theory is 《Novel pyrazolopyrimidines as highly potent B-Raf inhibitors》. Authors are Di Grandi, Martin J.; Berger, Dan M.; Hopper, Darrin W.; Zhang, Chunchun; Dutia, Minu; Dunnick, Alejandro L.; Torres, Nancy; Levin, Jeremy I.; Diamantidis, George; Zapf, Christoph W.; Bloom, Jonathan D.; Hu, YongBo; Powell, Dennis; Wojciechowicz, Donald; Collins, Karen; Frommer, Eileen.The article about the compound:3-(Pyridin-4-yl)-1H-pyrazol-5-aminecas:91912-53-7,SMILESS:NC1=CC(C2=CC=NC=C2)=NN1).Product Details of 91912-53-7. Through the article, more information about this compound (cas:91912-53-7) is conveyed.

A novel series of pyrazolo[1,5-a]pyrimidines bearing a 3-hydroxyphenyl group at C(3) and substituted tropanes at C(7) have been identified as potent B-Raf inhibitors. Exploration of alternative functional groups as a replacement for the C(3) phenol demonstrated indazole to be an effective isostere. Several compounds possessing substituted indazole residues, such as 4e, 4p, and 4r, potently inhibited cell proliferation at submicromolar concentrations in the A375 and WM266 cell lines, and the latter two compounds also exhibited good therapeutic indexes in cells.

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In general, if the atoms that make up the ring contain heteroatoms, such rings become heterocycles, and organic compounds containing heterocycles are called heterocyclic compounds. An article called Discovery of a novel alpha-7 nicotinic acetylcholine receptor agonist series and characterization of the potent, selective, and orally efficacious agonist 5-(4-Acetyl[1,4]diazepan-1-yl)pentanoic acid [5-(4-Methoxyphenyl)-1H-pyrazol-3-yl] amide (SEN15924, WAY-361789), published in 2012-05-24, which mentions a compound: 91912-53-7, Name is 3-(Pyridin-4-yl)-1H-pyrazol-5-amine, Molecular C8H8N4, Application In Synthesis of 3-(Pyridin-4-yl)-1H-pyrazol-5-amine.

Alpha-7 nicotinic acetylcholine receptors (α7 nAChR) are implicated in the modulation of many cognitive functions such as attention, working memory, and episodic memory. For this reason, α7 nAChR agonists represent promising therapeutic candidates for the treatment of cognitive impairment associated with Alzheimer’s disease (AD) and schizophrenia. A medicinal chem. effort, around our previously reported chem. series, permitted the discovery of a novel class of α7 nAChR agonists with improved selectivity, in particular against the α3 receptor subtype and better ADME profile. The exploration of this series led to the identification of 5-(4-acetyl[1,4]diazepan-1-yl)pentanoic acid [5-(4-methoxyphenyl)-1H-pyrazol-3-yl] amide [(I), SEN15924, WAY-361789], a novel, full agonist of the α7 nAChR that was evaluated in vitro and in vivo. Compound I proved to be potent and selective, and it demonstrated a fair pharmacokinetic profile accompanied by efficacy in rodent behavioral cognition models (novel object recognition and auditory sensory gating).

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Pyrazine – Wikipedia,
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Heterocyclic compounds can be divided into two categories: alicyclic heterocycles and aromatic heterocycles. Compounds whose heterocycles in the molecular skeleton cannot reflect aromaticity are called alicyclic heterocyclic compounds. Compound: 91912-53-7, is researched, Molecular C8H8N4, about Pyrazolo[1,5-a]pyrido[3,4-e]pyrimidin-6-ones. II. Synthesis and in vitro antimicrobial evaluation, the main research direction is pyrazolopyridopyrimidinone preparation bactericide fungicide; pyridopyrimidinone pyrazolo preparation bactericide fungicide; pyrimidinone pyrazolopyrido preparation bactericide fungicide.Application In Synthesis of 3-(Pyridin-4-yl)-1H-pyrazol-5-amine.

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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Yu, Ming; Lizarzaburu, Mike; Motani, Alykhan; Fu, Zice; Du, Xiaohui; Liu, Jiwen; Jiao, Xianyun; Lai, SuJen; Fan, Peter; Fu, Angela; Liu, Qingxiang; Murakoshi, Michiko; Nara, Futoshi; Oda, Kozo; Okuyama, Ryo; Reagan, Jeff D.; Watanabe, Nobuaki; Yamazaki, Mami; Xiong, Yumei; Zhang, Ying; Zhuang, Run; Lin, Daniel C.-H.; Houze, Jonathan B.; Medina, Julio C.; Li, Leping published the article 《Aminopyrazole-Phenylalanine Based GPR142 Agonists: Discovery of Tool Compound and in Vivo Efficacy Studies》. Keywords: amrinone phenylalanine carboxylic acid preparation GPR142 agonist structure design; pharmacokinetics bioavailability diabetes amrinone phenylalanine carboxylic acid antidiabetic prodrug; glucose tolerance insulin secretagogue human islet transplant CYP450 hERG; GPR142 agonist; aminopyrazole−phenylalanine; human islet transplant; insulin secretagogue; oral glucose tolerance test; prodrug; type 2 diabetes.They researched the compound: 3-(Pyridin-4-yl)-1H-pyrazol-5-amine( cas:91912-53-7 ).Reference of 3-(Pyridin-4-yl)-1H-pyrazol-5-amine. Aromatic heterocyclic compounds can be divided into two categories: single heterocyclic and fused heterocyclic. In addition, there is a lot of other information about this compound (cas:91912-53-7) here.

Herein, we report the lead optimization of amrinone-phenylalanine based GPR142 agonists. Structure-activity relationship studies led to the discovery of aminopyrazole-phenylalanine carboxylic acid I, which exhibited good agonistic activity, high target selectivity, desirable pharmacokinetic properties, and no cytochrome P 450 or hERG liability. Compound I, together with its orally bioavailable Et ester prodrug II, were found to be suitable for in vivo proof-of-concept studies. Compound II displayed good efficacy in a mouse oral glucose tolerance test (OGTT). CompoundI showed GPR142 dependent stimulation of insulin secretion in isolated mouse islets and demonstrated a statistically significant glucose lowering effect in a mouse model bearing transplanted human islets.

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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.Zanaletti, Riccardo; Bettinetti, Laura; Castaldo, Cristiana; Cocconcelli, Giuseppe; Comery, Thomas; Dunlop, John; Gaviraghi, Giovanni; Ghiron, Chiara; Haydar, Simon N.; Jow, Flora; Maccari, Laura; Micco, Iolanda; Nencini, Arianna; Scali, Carla; Turlizzi, Elisa; Valacchi, Michela researched the compound: 3-(Pyridin-4-yl)-1H-pyrazol-5-amine( cas:91912-53-7 ).Application In Synthesis of 3-(Pyridin-4-yl)-1H-pyrazol-5-amine.They published the article 《Discovery of a novel alpha-7 nicotinic acetylcholine receptor agonist series and characterization of the potent, selective, and orally efficacious agonist 5-(4-Acetyl[1,4]diazepan-1-yl)pentanoic acid [5-(4-Methoxyphenyl)-1H-pyrazol-3-yl] amide (SEN15924, WAY-361789)》 about this compound( cas:91912-53-7 ) in Journal of Medicinal Chemistry. Keywords: acetyldiazepanyl pentanoic acid methoxyphenyl pyrazolyl amide synthesis cholinergic agonist; nicotinic acetylcholine receptor agonist discovery structure activity mol docking. We’ll tell you more about this compound (cas:91912-53-7).

Alpha-7 nicotinic acetylcholine receptors (α7 nAChR) are implicated in the modulation of many cognitive functions such as attention, working memory, and episodic memory. For this reason, α7 nAChR agonists represent promising therapeutic candidates for the treatment of cognitive impairment associated with Alzheimer’s disease (AD) and schizophrenia. A medicinal chem. effort, around our previously reported chem. series, permitted the discovery of a novel class of α7 nAChR agonists with improved selectivity, in particular against the α3 receptor subtype and better ADME profile. The exploration of this series led to the identification of 5-(4-acetyl[1,4]diazepan-1-yl)pentanoic acid [5-(4-methoxyphenyl)-1H-pyrazol-3-yl] amide [(I), SEN15924, WAY-361789], a novel, full agonist of the α7 nAChR that was evaluated in vitro and in vivo. Compound I proved to be potent and selective, and it demonstrated a fair pharmacokinetic profile accompanied by efficacy in rodent behavioral cognition models (novel object recognition and auditory sensory gating).

There is still a lot of research devoted to this compound(SMILES：NC1=CC(C2=CC=NC=C2)=NN1)Application In Synthesis of 3-(Pyridin-4-yl)-1H-pyrazol-5-amine, and with the development of science, more effects of this compound(91912-53-7) can be discovered.

Reference:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

Most of the natural products isolated at present are heterocyclic compounds, so heterocyclic compounds occupy an important position in the research of organic chemistry. A compound: 91912-53-7, is researched, SMILESS is NC1=CC(C2=CC=NC=C2)=NN1, Molecular C8H8N4Journal, Article, ACS Medicinal Chemistry Letters called Aminopyrazole-Phenylalanine Based GPR142 Agonists: Discovery of Tool Compound and in Vivo Efficacy Studies, Author is Yu, Ming; Lizarzaburu, Mike; Motani, Alykhan; Fu, Zice; Du, Xiaohui; Liu, Jiwen; Jiao, Xianyun; Lai, SuJen; Fan, Peter; Fu, Angela; Liu, Qingxiang; Murakoshi, Michiko; Nara, Futoshi; Oda, Kozo; Okuyama, Ryo; Reagan, Jeff D.; Watanabe, Nobuaki; Yamazaki, Mami; Xiong, Yumei; Zhang, Ying; Zhuang, Run; Lin, Daniel C.-H.; Houze, Jonathan B.; Medina, Julio C.; Li, Leping, the main research direction is amrinone phenylalanine carboxylic acid preparation GPR142 agonist structure design; pharmacokinetics bioavailability diabetes amrinone phenylalanine carboxylic acid antidiabetic prodrug; glucose tolerance insulin secretagogue human islet transplant CYP450 hERG; GPR142 agonist; aminopyrazole−phenylalanine; human islet transplant; insulin secretagogue; oral glucose tolerance test; prodrug; type 2 diabetes.Application of 91912-53-7.

Herein, we report the lead optimization of amrinone-phenylalanine based GPR142 agonists. Structure-activity relationship studies led to the discovery of aminopyrazole-phenylalanine carboxylic acid I, which exhibited good agonistic activity, high target selectivity, desirable pharmacokinetic properties, and no cytochrome P 450 or hERG liability. Compound I, together with its orally bioavailable Et ester prodrug II, were found to be suitable for in vivo proof-of-concept studies. Compound II displayed good efficacy in a mouse oral glucose tolerance test (OGTT). CompoundI showed GPR142 dependent stimulation of insulin secretion in isolated mouse islets and demonstrated a statistically significant glucose lowering effect in a mouse model bearing transplanted human islets.

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