Month: April 2022

Related Products of 91912-53-7. 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 Novel pyrazolopyrimidines as highly potent B-Raf inhibitors.

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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Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

Product Details 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 Structure-activity relationship study, target identification, and pharmacological characterization of a small molecular IL-12/23 inhibitor, APY0201. Author is Hayakawa, Nobuhiko; Noguchi, Masatsugu; Takeshita, Sen; Eviryanti, Agung; Seki, Yukie; Nishio, Hikaru; Yokoyama, Ryohei; Noguchi, Misato; Shuto, Manami; Shima, Yoichiro; Kuribayashi, Kanna; Kageyama, Shunsuke; Eda, Hiroyuki; Suzuki, Manabu; Hatta, Tomohisa; Iemura, Shun-ichiro; Natsume, Tohru; Tanabe, Itsuya; Nakagawa, Ryusuke; Shiozaki, Makoto; Sakurai, Kuniya; Shoji, Masataka; Andou, Ayatoshi; Yamamoto, Takashi.

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.

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Pyrazine – Wikipedia,
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Electric Literature of C4H5N3. The mechanism of aromatic electrophilic substitution of aromatic heterocycles is consistent with that of benzene. Compound: 4-Aminopyrimidine, is researched, Molecular C4H5N3, CAS is 591-54-8, about Study on hydrothermal liquefaction of spirulina platensis using biochar based catalysts to produce bio-oil. Author is Wang, Bin; He, Zhixia; Zhang, Bo; Duan, Yibing.

Hydrothermal liquefaction (HTL) is an effective conversion technol. of microalgae biomass. In this study, the low-lipid microalgae-spirulina platensis was used as feedstock to investigate the performance of the biochar-based catalysts on HTL. The byproduct of spirulina platensis HTL-solid residue was collected and activated to obtain the biochar (BC). Then, the BC was used as the carrier to support Co, Ni and their oxides CoOx and NiO to form Co/BC, Ni/BC, CoOx/BC, NiO/BC catalysts. The Response Surface Methodol. (RSM) was used to optimize the HTL parameters and investigate the effect of biochar-based catalysts on HTL. The results showed that the maximum yield of bio-oil catalyzed by BC was 35.80 wt% with 304 °C, 34.7 min, and 0.32 g catalyst loading. BC catalyst displayed an improvement of bio-oil yield up to 4.00 wt% at low temperatures (260-280 °C). Ni/BC was the most favorable catalyst for bio-oil production, reaching a maximum value of 36.57 wt% at 280 °C, 35.0 min, and 0.15 g catalyst loading, which increased by 6.40 wt% compared with the non catalytic case. The characterization of bio-oil showed that CoOx/BC and NiO/BC could raise the hydrocarbon content, H/C value, and heat value, while decrease O/C value. Ni/BC had an excellent denitrification effect on bio-oil, the N content was reduced by nearly 2.00 wt% compared with the non catalytic case.

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Singh, Baljinder; Diaz-Gonzalez, Rosario; Ceballos-Perez, Gloria; Rojas-Barros, Domingo I.; Gunaganti, Naresh; Gillingwater, Kirsten; Martinez-Martinez, Maria Santos; Manzano, Pilar; Navarro, Miguel; Pollastri, Michael P. published the article 《Medicinal Chemistry Optimization of a Diaminopurine Chemotype: Toward a Lead for Trypanosoma brucei Inhibitors》. Keywords: diaminopurine chemotype optimization preparation Trypanosoma brucei structure.They researched the compound: 4-Aminopyrimidine( cas:591-54-8 ).Name: 4-Aminopyrimidine. 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:591-54-8) here.

Human African trypanosomiasis (HAT), or sleeping sickness, is caused by the protozoan parasite Trypanosoma brucei and transmitted through the bite of infected tsetse flies. The disease is considered fatal if left untreated. To identify new chemotypes against Trypanosoma brucei, previously we identified 797 potent kinase-targeting inhibitors grouped into 59 clusters plus 53 singleton compounds with at least 100-fold selectivity over HepG2 cells. From this set of hits, a cluster of diaminopurine-derived compounds was identified. Herein, we report our medicinal chem. investigation involving the exploration of structure-activity and structure-property relationships around one of the high-throughput screening (HTS) hits, N2-(thiophen-3-yl)-N6-(2,2,2-trifluoroethyl)-9H-purine-2,6-diamine (1, NEU-1106). This work led to the identification of a potent lead compound (4aa, NEU-4854) with improved in vitro absorption, distribution, metabolism, and excretion (ADME) properties, which was progressed into proof-of-concept translation of in vitro antiparasitic activity to in vivo efficacy.

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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: 2150-55-2, is researched, Molecular C4H6N2O2S, about Isolation and genetic improvement of Pseudomonas sp. strain HUT-78, capable of enzymatic production of L-cysteine from DL-2-amino-Δ2-thiazoline-4-carboxylic acid, the main research direction is cysteine production Pseudomonas fermentation mutagenesis genetic engineering; aminothiazolinecarboxylate hydrolase carbamoylcysteine amidohydrolase Pseudomonas.HPLC of Formula: 2150-55-2.

Microorganisms able to bioconvert DL-2-amino-Δ2-thiazoline-4-carboxylic acid (DL-ATC) into L-cysteine were originally isolated from 10 soil samples with DL-ATC as the sole nitrogen source. Ninety-seven L-cysteine-producing bacterial strains were screened out and obtained in pure culture. Among them, a strain, designated as HUT-78, was selected as the best producer, with a molar bioconversion rate of 60%. Based on the 16S rRNA gene sequence anal., this isolate was placed within the genus Pseudomonas. A novel mutant of this strain with a significantly reduced activity of L-cysteine desulfhydrase, a L-cysteine-decomposing enzyme, was derived by UV-mutagenesis. This mutant, designated as mHUT-78, exhibited a 42% increase in L-cysteine producing activity. Moreover, the bioconversion reactions in both the parent and the mutant strain were significantly accelerated by co-overexpression of the two key enzymes, AtcB and AtcC, involved in the bioconversion reaction.

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Pyrazine – Wikipedia,
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Application of 118994-89-1. 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: Ethyl oxazole-5-carboxylate, is researched, Molecular C6H7NO3, CAS is 118994-89-1, about Asymmetric Alkyl and Aryl/Azolation of Alkenes via a Single Cu(I) Complex. Author is Ma, Xiaodong; Zhang, Guozhu.

The copper-catalyzed, highly enantioselective alkyl and aryl/azolation of alkenes was reported. The employment of the chiral carbazole-based bisoxazoline (Cbzbox) ligand was critical to the success of this chem. Anionic tridentate ligands improved the reducibility of copper complexes, facilitating alkyl/aryl radical generation and provided good enantiocontrol in the azolation. The three-component coupling reactions featured mild reaction conditions and tolerate broad range of functional groups. This strategy allowed straightforward introduction of valuable azole functionalities into a elaborated mol. system through direct C-H functionalization.

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Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

Category: pyrazines. 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: 2-Amino-4,5-dihydrothiazole-4-carboxylic acid, is researched, Molecular C4H6N2O2S, CAS is 2150-55-2, about Study on fermentation conditions and culture medium of enzymatic synthesis of L-cysteine. Author is Kou, Guang-hui; Zhou, Chang-ping; Liu, Shu-yun; Chen, Ning.

L-cysteine synthesizing enzyme could be produced in Pseudomonas sp.TS1138, induced by DL-2-amino-Δ2-thiazoline-4-carboxylic acid (DL-ATC). Optimum conditions suitable for enzyme production in Pseudomonas sp. TS1138 were studied and the results showed that enzymes activity in Pseudomonas sp. TS1138 was highest when the cultivate conditions were as follows: mass concentration of DL-ATC was 5 g/L, glucose and urea were carbon and nitrogen source resp., fermentation temperature was 27-29°C, liquid volume of culture medium was 40 mL in a 500 mL shaking flask. The highest enzymes activity could reach 1,780 U/mL in a 7 L fermentor under the optimum conditions.

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Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

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 Soluble-type small-molecule CD4 mimics as HIV entry inhibitors, published in 2019-03-01, which mentions a compound: 1827-27-6, Name is 5-Amino-2-fluoropyridine, Molecular C5H5FN2, Computed Properties of C5H5FN2.

Several small mol. CD4 mimics have been reported previously as HIV-1 entry inhibitors, which block the interaction between the Phe43 cavity of HIV-1 gp120 and the host CD4. Known CD4 mimics such as NBD-556 possess significant anti-HIV activity but are less soluble in water, perhaps due to their hydrophobic aromatic ring-containing structures. Compounds with a pyridinyl group in place of the Ph group in these mols. have been designed and synthesized in an attempt to increase the hydrophilicity. Some of these new CD4 mimics, containing a tetramethylpiperidine ring show significantly higher water solubility than NBD-556 and have high anti-HIV activity and synergistic anti-HIV activity with a neutralizing antibody. The CD4 mimic that has a cyclohexylpiperidine ring and a 6-fluoropyridin-3-yl ring has high anti-HIV activity and no significant cytotoxicity. The present results will be useful in the future design and development of novel soluble-type mol. CD4 mimics.

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Pyrazine – Wikipedia,
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Recommanded Product: 121816-79-3. 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: 4-Bromo-1-methyl-2-nitro-1H-imidazole, is researched, Molecular C4H4BrN3O2, CAS is 121816-79-3, about Synthesis and reactions of brominated 2-nitroimidazoles.

Imidazoles reacted with N-bromosuccinimide to give 4-bromo derivatives I (R1 = H, Me, CPh3; R2 = H, NO2, Me). 2-Nitroimidazole gave dibromo compound II as the only product. I (R1 = CPh3, R2 = H) was treated with BuLi, PrONO2, and HCl to give I (R1 = H, R2 = NO2).

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Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

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, General Review, Article, Review, Molecules called Synthetic Strategies of Pyrimidine-Based Scaffolds as Aurora Kinase and Polo-like Kinase Inhibitors, Author is Jadhav, Mrunal; Sankhe, Kaksha; Bhandare, Richie R.; Edis, Zehra; Bloukh, Samir Haj; Khan, Tabassum Asif, which mentions a compound: 591-54-8, SMILESS is C1=CN=CN=C1N, Molecular C4H5N3, Related Products of 591-54-8.

A review. Small mols. containing heterocyclic moieties have attracted considerable interest for designing new antitumor agents. Of these, the pyrimidine ring system is found in multitude of drug structures, and being the building unit of DNA and RNA makes it an attractive scaffold for the design and development of anticancer drugs. Currently, 22 pyrimidine-containing entities are approved for clin. use as anticancer drugs by the FDA. An exhaustive literature search indicates several publications and more than 59 patents from the year 2009 onwards on pyrimidine derivatives exhibiting potent antiproliferative activity. These pyrimidine derivatives exert their activity via diverse mechanisms, one of them being inhibition of protein kinases. Aurora kinase (AURK) and polo-like kinase (PLK) are protein kinases involved in the regulation of the cell cycle. Within the numerous pyrimidine-based small mols. developed as anticancer agents, this review focuses on the pyrimidine fused heterocyclic compounds modulating the AURK and PLK proteins in different phases of clin. trials as anticancer agents. This article aims to provide a comprehensive overview of synthetic strategies for the preparation of pyrimidine derivatives and their associated biol. activity on AURK/PLK. It will also present an overview of the synthesis of the heterocyclic-2-aminopyrimidine, 4-aminopyrimidine and 2,4-diaminopyrimidine scaffolds, and one of the pharmacophores in AURK/PLK inhibitors is described systematically.

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Pyrazine – Wikipedia,
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