Month: April 2022

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 Synthesis and hypoxia-selective cytotoxicity of a 2-nitroimidazole mustard, published in 1998-07-07, which mentions a compound: 121816-79-3, mainly applied to chloroethylaminonitroimidazole preparation hypoxia selective cytotoxicity; nitroimidazole mustard preparation hypoxia selective cytotoxicity; imidazole chloroethylaminonitro preparation hypoxia selective cytotoxicity, Product Details of 121816-79-3.

A four-step synthesis of 5-[N,N-bis(2-chloroethyl)amino]-1-methyl-2-nitroimidazole from 1-methyl-2-nitroimidazole is described. This compound showed similar hypoxia-selective cytotoxicity to the dinitrobenzamide mustard SN 23862 in UV4 cells (ca. 40-fold), and superior selectivity (>7-fold) in repair-competent AA8 cells.

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Reference:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

The chemical properties of alicyclic heterocycles are similar to those of the corresponding chain compounds. Compound: 4-Aminopyrimidine, is researched, Molecular C4H5N3, CAS is 591-54-8, about Recent developments of RET protein kinase inhibitors with diverse scaffolds as hinge binders, the main research direction is review RET protein kinase inhibitor nicotinonitrile imidazopyridazine pyridone; RET; RET inhibitors; RET mutation; RET-driven cancers; hinge binder; precision targeted therapy.Computed Properties of C4H5N3.

A review. RET is a proto-oncogene encoding a receptor tyrosine kinase. RET regulates key aspects of cellular proliferation, differentiation and survival. The activation of RET via gene fusions or point mutations is closely related to lung, thyroid and other cancers. This review summarizes the developments of a diversity of small mol. RET protein kinase inhibitors in the past 10 years. These RET inhibitors are classified according to their hinge binder chemotypes as: pyrimidines, including the pyrazolopyrimidines, pyrimidine oxazines, quinazolines, 4-aminopyrimidines and 4-aminopyridines; indolinones; 5-aminopyrazole-4-carboxamides; 3-trifluoromethylanilines; imidazopyridines, imidazopyridazines and pyrazopyridines; nicotinonitriles; pyridones and 1,2,4-triazoles. In each section, the biol. activities of the inhibitors, their structure-activity relationships and possible binding modes with the RET kinase are introduced.

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Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

Edney, Dean; Hulcoop, David G.; Leahy, John H.; Vernon, Lois E.; Wipperman, Mark D.; Bream, Robert N.; Webb, Michael R. published an article about the compound: Ethyl oxazole-5-carboxylate( cas:118994-89-1,SMILESS:O=C(C1=CN=CO1)OCC ).Quality Control of Ethyl oxazole-5-carboxylate. 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:118994-89-1) through the article.

This paper describes the discovery and development of a flexible route to two candidate drug mols. by a common intermediate approach. Key reactions include Negishi and Suzuki couplings to form biaryl bonds. Conditions for a Miyaura borylation of heteroaryl bromides were also developed. Heteroaryl trifluoroborates and aryl chlorides were used as coupling partners in the Suzuki reaction, thereby minimizing detrimental side reactions such as protodeboronation and oxidative homocoupling. A complementary set of reaction conditions using pinacolboronates with potassium bifluoride as an additive were also developed and used to make 5 kg of drug substance for use in early-phase clin. trials.

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Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

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: 591-54-8, is researched, Molecular C4H5N3, about Design, synthesis and evaluation of novel 9-arylalkyl-10-methylacridinium derivatives as highly potent FtsZ-targeting antibacterial agents, the main research direction is arylalkyl methylacridinium preparation antibacterial SAR mol docking; 9-Arylalkyl-10-methylacridinium derivatives; Antibacterial activity; Design and synthesis; FtsZ inhibitor; Structure-activity relationships.Name: 4-Aminopyrimidine.

With the increasing incidence of antibiotic resistance, new antibacterial agents having novel mechanisms of action hence are in an urgent need to combat infectious diseases caused by multidrug-resistant (MDR) pathogens. Four novel series of substituted 9-arylalkyl-10-methylacridinium derivatives as FtsZ inhibitors were designed, synthesized and evaluated for their antibacterial activities against various Gram-pos. and Gram-neg. bacteria. The results demonstrated that they exhibited broad-spectrum activities with substantial efficacy against MRSA and VRE, which were superior or comparable to the berberine, sanguinarine, linezolid, ciprofloxacin and vancomycin. In particular, the most promising compound I showed rapid bactericidal properties, which avoid the emergence of drug resistance. However, I showed no inhibitory effect on Gram-neg. bacteria but biofilm formation study gave possible answers. Further target identification and mechanistic studies revealed that I functioned as an effective FtsZ inhibitor to alter the dynamics of FtsZ self-polymerization, which resulted in termination of the cell division and caused cell death. Further cytotoxicity and animal studies demonstrated that I not only displayed efficacy in a murine model of bacteremia in vivo, but also no significant hemolysis to mammalian cells. Overall, this compound with novel skeleton could serve as an antibacterial lead of FtsZ inhibitor for further evaluation of drug-likeness.

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Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

Electric Literature of C5H5FN2. 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: 5-Amino-2-fluoropyridine, is researched, Molecular C5H5FN2, CAS is 1827-27-6, about Design, Synthesis, and Structure-Activity Relationship of Indole-3-glyoxylamide Libraries Possessing Highly Potent Activity in a Cell Line Model of Prion Disease. Author is Thompson, Mark J.; Borsenberger, Vinciane; Louth, Jennifer C.; Judd, Katie E.; Chen, Beining.

Transmissible spongiform encephalopathies (TSEs) are a family of invariably fatal neurodegenerative disorders for which no effective curative therapy currently exists. We report here the synthesis of a library of indole-3-glyoxylamides and their evaluation as potential antiprion agents. A number of compounds demonstrated submicromolar activity in a cell line model of prion disease together with a defined structure-activity relationship, permitting the design of more potent compounds that effected clearance of scrapie in the low nanomolar range. Thus, the indole-3-glyoxylamides described herein constitute ideal candidates to progress to further development as potential therapeutics for the family of human prion disorders.

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Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

Name: 4-Aminopyrimidine. 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 Design, synthesis and biological evaluation of pyridone-aminal derivatives as MNK1/2 inhibitors. Author is Yuan, Xinrui; Wu, Hanshu; Bu, Hong; Zheng, Peiyuan; Zhou, Jinpei; Zhang, Huibin.

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.

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Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

Epoxy compounds usually have stronger nucleophilic ability, because the alkyl group on the oxygen atom makes the bond angle smaller, which makes the lone pair of electrons react more dissimilarly with the electron-deficient system. Compound: Ethyl oxazole-5-carboxylate, is researched, Molecular C6H7NO3, CAS is 118994-89-1, about A general route to the Streptomyces-derived inthomycin family: the first synthesis of (+)-inthomycin B.Safety of Ethyl oxazole-5-carboxylate.

A concise, convergent and stereocontrolled synthesis of (+)-inthomycin B (I), based on the Stille coupling of a stannyl-diene with an oxazole vinyl iodide unit, is described. The asym. center was introduced using the Kiyooka ketene acetal/amino acid-derived oxazaborolidinone procedure.

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Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

HPLC of Formula: 1827-27-6. 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: 5-Amino-2-fluoropyridine, is researched, Molecular C5H5FN2, CAS is 1827-27-6, about Solvent and substituent effects on fluorine-19 chemical shifts in some 5-substituted 2-fluoropyridines. Author is Giam, Choo-Seng; Lyle, James L..

The 19F NMR chem. shifts of several 5-substituted 2-fluoropyridines in 4 widely different solvents have been measured. The effects of solvents and substituents on the shifts paralleled those in the benzene series with certain modifications.

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Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

Formula: C4H6N2O2S. 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 Progress on enzymatic synthesis of L-cysteine from DL-ATC by Pseudomonas sp.. Author is Wu, Min; Chen, Wei-qing; Wang, Pu; He, Jun-yao.

A review. The microbial transformation method for L-cysteine production shows evident advantages, because of its short cycle time, low cost, high region and stereoselectivity, easy control of reaction condition, and environment-friendly. Recently, studies on the bioconversion of DL-2-amino-Δ2-thiazoline-4-carboxylic acid (DL-ATC) to L-cysteine by intracellular enzymes were reported. The research progresses on L-cysteine production by microbial bioconversion, especially Pseudomonas sp., or its crude enzyme extract are summarized. The applications of immobilization technol. in the biotransformation of DL-ATC to L-cysteine are introduced. The genetically engineered bacteria and the study progresses of L-cysteine desulfhydrase were also discussed.

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Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

Recommanded Product: 5-Amino-2-fluoropyridine. The mechanism of aromatic electrophilic substitution of aromatic heterocycles is consistent with that of benzene. Compound: 5-Amino-2-fluoropyridine, is researched, Molecular C5H5FN2, CAS is 1827-27-6, about Design, synthesis of novel celastrol derivatives and study on their antitumor growth through HIF-1α pathway. Author is Shang, Fan-Fan; Wang, Jing Ying; Xu, Qian; Deng, Hao; Guo, Hong-Yan; Jin, Xuejun; Li, Xiaoting; Shen, Qing-Kun; Quan, Zhe-Shan.

Four series of hypoxia-inducible factor-1 alpha (HIF-1α) functioning derivatives stemming from modifications to the C-29 carboxyl group of celastrol were designed and synthesized, and their anticancer activities were evaluated. To address the structure and activity relationship of each derivative, extensive structural changes were made. HRE luciferase reporter assay demonstrated that 12 modified compounds showed superior HIF-1α inhibitory activity. Among them, quinolin-7-yloxy derivative I exhibited the best features: first, it had the strongest HIF-1α inhibitory activity (IC50 = 0.05μM, 5-fold higher than that of celastrol), and second, it possessed lower cytotoxicity (22-fold lower, I 16.85μM vs. celastrol 0.76μM). Thus, the safety factor of C6 was about 112 times higher than that of celastrol. Western blot assay indicated that I may inhibit the expression of HIF-1α protein in cells. Addnl., I hindered tumor cell cloning, migration and induced cell apoptosis. It is worth mentioning that in the mouse tumor xenograft model, I (10 mg/kg) displayed good antitumor activity in vivo, showing a better inhibition rate (74.03%) than the reference compound 5-fluorouracil (inhibition rate, 59.58%). However, the celastrol treatment group experienced collective death after four doses of the drug. Moreover, I minimally affected the mouse weight, indicating that its application in vivo has little toxic effect. H&E staining experiments show that it could also exacerbate the degree of tumor cell damage. The results of water solubility experiment show that the solubility of I is increased by 1.36 times than that of celastrol. In conclusion, I is a promising antitumor agent through the HIF-1α pathway.

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Reference:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem