Category: 591-54-8

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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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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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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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 Antioxidative study of polysaccharides extracted from red (Kappaphycus alvarezii), green (Kappaphycus striatus) and brown (Padina gymnospora) marine macroalgae/seaweed, the main research direction is Kappaphycus Padina Gracilaria antioxidant polysaccharide.Application In Synthesis of 4-Aminopyrimidine.

Sterile and fresh tissues of three marine macroalgae red, green and brown (Kappaphycus alvarezii, Kappaphycus striatus and Padina gymnospora) collected from Malaysia east costal seas were compared for the antioxidants and polysaccharide composition of sugars as well as the active components. Results obtained showed that polysaccharides isolated from Kappaphycus alvarezii, Kappaphycus striatus and Padina gymnospora) can be used as a source of natural antioxidant compounds as they possess antioxidant potential in which the Padina gymnospora showed 15.56 ± 0.12 mg/mL to be the best antioxidants among all the polysaccharides studied. The hot water extraction method is effective in isolating polysaccharides from studied seaweeds. The GC-MS anal. revealed that there is presence of chem. compounds such as furfural was 25.53% in Kappaphycus alvarezii and 21.04% in Kappaphycus striatus also Padina gymnospora incorporates n- Hexadecanoic acid about 26.31% in seaweed polysaccharides that contribute to their antioxidant activities. Further studies can be done on determining the seaweed species that are available abundantly with the best source of natural antioxidant compounds

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Wu, Peng; Bjoern-Yoshimoto, Walden E.; Staudt, Markus; Jensen, Anders A.; Bunch, Lennart published an article about the compound: 4-Aminopyrimidine( cas:591-54-8,SMILESS:C1=CN=CN=C1N ).HPLC of Formula: 591-54-8. 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:591-54-8) through the article.

Screening of a library of 49,087 compounds at the excitatory amino acid transporter subtype 3 (EAAT3) led to the identification of 2-(furan-2-yl)-8-methyl-N-(o-tolyl)imidazo[1,2-a]pyridin-3-amine which showed a >20-fold preference for inhibition of EAAT3 (IC50 = 13 μM) over EAAT1,2,4 (EAAT1: IC50 ∼ 250 μM; EAAT2,4: IC50 > 250 μM). A small lipophilic substituent (Me or bromine) at the 7- and/or 8-position was essential for activity. Furthermore, the substitution pattern of the o-tolyl group (compound I) and the chem. nature of the substituent in the 2-position of tert-Bu 3-(8-bromo-7-methyl-3-(o-tolylamino)imidazo[1,2-a]pyridin-2-yl)azetidine-1-carboxylate are essential for the selectivity toward EAAT3 over EAAT1,2. The most prominent analogs to come out of this study are 2-(furan-2-yl)-8-methyl-N-(o-tolyl)imidazo[1,2-a]pyridin-3-amine and 8-Bromo-2-(furan-2-yl)-N-(o-tolyl)imidazo[1,2-a]pyridin-3-amine that display ∼35-fold selectivity for EAAT3 (IC50 = 7.2 μM) over EAAT1,2,4 (IC50 ∼ 250 μM).

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Fang, Zhennan; Wei, Huiqiang; Gou, Wenfeng; Chen, Leyuan; Bi, Changfen; Hou, Wenbin; Li, Yiliang published an article about the compound: 4-Aminopyrimidine( cas:591-54-8,SMILESS:C1=CN=CN=C1N ).Recommanded Product: 4-Aminopyrimidine. 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:591-54-8) through the article.

A review. Nonapoptotic types of regulated cell death have attracted widespread interest since the discovery that certain forms of cell necrosis can be regulated. In particular, research into cell necroptosis has made significant progress in connection with kidney, inflammatory, degenerative and neoplastic diseases. Inhibitors targeting the critical necroptosis-associated proteins RIPK1/3 and MLKL have been in development for more than a decade. Herein the authors compile a list of the known small-mol. inhibitors of these enzymes and representative structures of compounds co-crystallized with these proteins and put forward some thoughts regarding their future development.

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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 Dual Tubulin Polymerization and Cell Division Cycle 20 Homologue Inhibitor via Structural Modification on Apcin, published in 2020-05-14, which mentions a compound: 591-54-8, Name is 4-Aminopyrimidine, Molecular C4H5N3, Category: pyrazines.

Apcin is one of the few compounds that have been previously reported as a Cdc20 specific inhibitor, although Cdc20 is a very promising drug target. We reported here the design, synthesis, and biol. evaluations of 2,2,2-trichloro-1-aryl carbamate derivatives as Cdc20 inhibitors. Among these derivatives, compound 9f(I) was much more efficient than the pos. compound apcin in inhibiting cancer cell growth, but it had approx. the same binding affinity with apcin in SPR assays. It is possible that another mechanism of action might exist. Further evidence demonstrated that compound 9f also inhibited tubulin polymerization, disorganized the microtubule network, and blocked the cell cycle at the M phase with changes in the expression of cyclins. Thus, it induced apoptosis through the activation of caspase-3 and PARP. In addition, compound 9f inhibited cell migration and invasion in a concentration-dependent manner. These results provide guidance for developing the current series as potential new anticancer therapeutics.

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Yu, Bin; Zhao, Bin; Hao, Zesheng; Chen, Lei; Cao, Lixin; Guo, Xiaofeng; Zhang, Nailou; Yang, Dongyan; Tang, Liangfu; Fan, Zhijin published the article 《Design, synthesis and biological evaluation of pyrazole-aromatic containing carboxamides as potent SDH inhibitors》. Keywords: pyrazole thiazole aryl carboxamide preparation antifungal SDH inhibitor SAR; Antifungal activity; Molecular docking; Structure-activity relationships; Succinate dehydrogenase inhibitors.They researched the compound: 4-Aminopyrimidine( cas:591-54-8 ).Category: pyrazines. 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.

To continue studies on discovery of new potent antifungal leads, 43 novel pyrazole-aromatic containing carboxamides were rationally designed and synthesized. Bioassays indicated that most target compounds displayed good in vitro antifungal activities against Botrytis cinerea, Rhizoctonia cerealis and Sclerotinia sclerotiorum and in vivo antifungal activity against R. solani. Compound I exhibited the most significant in vitro activity against R. cerealis (EC50 = 0.93μg/mL) with about 2-fold more potent than a previously reported lead compound N-(3-bromophenyl)-2-[3-(difluoromethyl)-1-methyl-1H-pyrazol-4-yl]-4-thiazolecarboxamide (EC50 = 2.01μg/mL), and about 11-fold more potent than the pos. control/com. succinate dehydrogenase inhibitor thifluzamide (EC50 = 23.09μg/mL). Structure-activity relationship anal. and mol. docking simulations indicated that the presence of difluoromethyl pyrazole-(m-benzene)carboxamide scaffold obviously increased the antifungal activity. The further enzymic bioassay showed that both thifluzamide and compound I displayed excellent SDH inhibitory effects, and fluorescence quenching anal. suggested that they may share the same target SDH.

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The three-dimensional configuration of the ester heterocycle is basically the same as that of the carbocycle. Compound: 4-Aminopyrimidine(SMILESS: C1=CN=CN=C1N,cas:591-54-8) is researched.Application In Synthesis of 2-Amino-4,5-dihydrothiazole-4-carboxylic acid. The article 《Spectrum of antiviral activity of 4-aminopyrimidine N-oxides against a broad panel of tick-borne encephalitis virus strains》 in relation to this compound, is published in Antiviral Chemistry and Chemotherapy. Let’s take a look at the latest research on this compound (cas:591-54-8).

Tick-borne encephalitis is an important human arbovirus neuroinfection spread across the Northern Eurasia. Inhibitors of tick-borne encephalitis virus (TBEV) strain Absettarov, presumably targeting E protein n-octyl-β-D-glucoside (β-OG) pocket, were reported earlier. In this work, these inhibitors were tested in vitro against seven strains representing three main TBEV subtypes. The most potent compound, 2-[(2-methyl-1-oxido-5,6,7,8-tetrahydroquinazolin-4-yl)amino]-phenol, showed EC50 values lower than 22 μM against all the tested strains. Nevertheless, EC50 values for virus samples of certain strains demonstrated a substantial variation, which appeared to be consistent with the presence of E protein not only in infectious virions, but also in non-infectious and immature virus particles, protein aggregates, and membrane complexes.

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The reaction of an aromatic heterocycle with a proton is called a protonation. One of articles about this theory is 《Controlling Two-Photon Action Cross Section by Changing a Single Heteroatom Position in Fluorescent Dyes》. Authors are Osmialowski, Borys; Petrusevich, Elizaveta F.; Antoniak, Magda A.; Grela, Izabela; Bin Jassar, Mohammed A.; Nyk, Marcin; Luis, Josep M.; Jedrzejewska, Beata; Zalesny, Robert; Jacquemin, Denis.The article about the compound:4-Aminopyrimidinecas:591-54-8,SMILESS:C1=CN=CN=C1N).Formula: C4H5N3. Through the article, more information about this compound (cas:591-54-8) is conveyed.

The optimization of nonlinear optical properties for “”real-life”” applications remains a key challenge for both exptl. and theor. approaches. In particular, for two-photon processes, maximizing the two-photon action cross section (TPACS), the figure of merit for two-photon bioimaging spectroscopy, requires simultaneously controlling all its components. In the present Letter, a series of difluoroborates presenting various heterocyclic rings as an electron acceptor have been synthesized and their absorption, fluorescence, photoisomerization, and two-photon absorption features have been analyzed using both exptl. and theor. approaches. Our results demonstrate that the TPACS values can be fine-tuned by changing the position of a single heteroatom, which alters the fluorescence quantum yields without changing the intrinsic two-photon absorption cross section. This approach offers a new strategy for optimizing TPACS.

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