Tag: 100-200

Stahlberger, M.; Steinlein, O.; Adam, C. R.; Rotter, M.; Hohmann, J.; Nieger, M.; Koeberle, B.; Braese, S. published an article in 2022. The article was titled 《Fluorescent annulated imidazo[4,5-c]isoquinolines via a GBB-3CR/imidoylation sequence – DNA-interactions in pUC-19 gel electrophoresis mobility shift assay》, and you may find the article in Organic & Biomolecular Chemistry.Electric Literature of C6H4BrNO The information in the text is summarized as follows:

The development of a sequential synthesis route towards annulated imidazo[4,5-c]isoquinolines comprising a GBB-3CR, followed by an intramol. imidoylative cyclization was reported. X-Ray crystallog. revealed a flat 3D structure of the obtained polyheterocycles. Thus, their interactions with double-stranded DNA was evaluated by establishing a pUC-19 plasmid-based gel electrophoresis mobility shift assay, revealing a stabilizing effect on ds-DNA against strand-break inducing conditions.2-Bromonicotinaldehyde(cas: 128071-75-0Electric Literature of C6H4BrNO) was used in this study.

2-Bromonicotinaldehyde(cas: 128071-75-0) belongs to pyridine. Pyridine is widely used in the precursor to agrochemicals and pharmaceuticals. Also, it is used as an important reagent and organic solvent.Electric Literature of C6H4BrNO

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Lu, Fangjie; Xu, Dong; Lu, Yusheng; Dai, Bin; Zhu, Mingyuan published an article in 2021. The article was titled 《High nitrogen carbon material with rich defects as highly efficient metal-free catalyst for excellent catalytic performance of acetylene hydrochlorination》, and you may find the article in Chinese Journal of Chemical Engineering.Product Details of 141-86-6 The information in the text is summarized as follows:

In this work, we developed a simple strategy to synthesize a carbon material with high nitrogen and rich carbon defects. Our approach polymerized diaminopyridine (DAP) and ammonium persulfate (APS). Following a range of different temperature pyrolysis approaches, the resulting rough surface was shown to exhibit edge defects due to N-doping on graphite carbon. A series of catalysts were evaluated using a variety of characterization techniques and tested for catalytic performance. The catalytic performance of the N-doped carbon material enhanced alongside an increment in carbon defects. The NC-800 catalyst exhibited outstanding catalytic activity and stability in acetylene hydrochlorination (C2H2 GHSV = 30 h-1, at 220 °C, the acetylene conversion rate was 98%), with its stability reaching up to 450 h. Due to NC-800 having a nitrogen content of up to 13.46%, it had the largest sp. surface area and a high defect amount, as well as strong C2H2 and HCl adsorption. NC-800 has excellent catalytic activity and stability to reflect its unlimited potential as a carbon material. In addition to this study using 2,6-Diaminopyridine, there are many other studies that have used 2,6-Diaminopyridine(cas: 141-86-6Product Details of 141-86-6) was used in this study.

2,6-Diaminopyridine(cas: 141-86-6) belongs to pyridine. Pyridine and its simple derivatives are stable and relatively unreactive liquids, with strong penetrating odours that are unpleasant.Product Details of 141-86-6

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Xu, Mizhi; Paul, McKinley K.; Bullard, Krista K.; DuPre, Christopher; Gutekunst, Will R. published an article in 2021. The article was titled 《Modulating Twisted Amide Geometry and Reactivity Through Remote Substituent Effects》, and you may find the article in Journal of the American Chemical Society.SDS of cas: 1692-25-7 The information in the text is summarized as follows:

The unusual reactivity of twisted amides has long been associated with the degree of amide distortion, though classical bridged bicyclic amides offer limited methods to further modify these parameters. Here, we report that the geometry and reactivity of a single twisted amide scaffold can be significantly modulated through remote substituent effects. Guided by calculated ground state geometries, a library of twisted amide derivatives was efficiently prepared through a divergent synthetic strategy. Kinetic and mechanistic investigations of these amides in the alkylation/halide-rebound ring-opening reaction with alkyl halides show a strong pos. correlation between the electron donating ability of the substituent and distortion of the amide bond, leading to rates of nucleophilic substitution spanning nearly 2 orders of magnitude. The rate limiting step of the cascade sequence is found to be dependent on the nature of the substituent, and addnl. studies highlight the role of solvent polarity and halide ion on reaction pathway and efficiency. The experimental part of the paper was very detailed, including the reaction process of Pyridin-3-ylboronic acid(cas: 1692-25-7SDS of cas: 1692-25-7)

Pyridin-3-ylboronic acid(cas: 1692-25-7) belongs to pyridine. When pyridine is adsorbed on oxide surfaces or in porous materials, the following species are commonly observed: (i) pyridine coordinated to Lewis acid sites, (ii) pyridine H-bonded to weakly acidic hydroxyls, and (iii) protonated pyridine. At high coverage, physisorbed pyridine and protonated dimers can also be observed.SDS of cas: 1692-25-7

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Liu, Wenwu; Liu, Xin; Tian, Liting; Gao, Yaping; Liu, Wenjie; Chen, Huanhua; Jiang, Xiaowen; Xu, Zihua; Ding, Huaiwei; Zhao, Qingchun published an article in 2021. The article was titled 《Design, synthesis and biological evaluation of harmine derivatives as potent GSK-3β/DYRK1A dual inhibitors for the treatment of Alzheimer’s disease》, and you may find the article in European Journal of Medicinal Chemistry.HPLC of Formula: 1692-25-7 The information in the text is summarized as follows:

Alzheimer’s disease (AD) is a chronic and progressive neurodegenerative disease, characterized by irreversible cognitive impairment, memory loss and behavioral disturbances, ultimately leading to death. Glycogen synthase kinase 3β (GSK-3β) and dual-specificity tyrosine phosphorylation regulated kinase1A (DYRK1A) have gained a lot of attention for its role in tau pathol. To search for potential dual GSK-3β/DYRK1A inhibitors, we focused on harmine, a natural β-carboline alkaloid, which has been extensively studied for its various biol. effects on the prevention of AD. In this study, a new series of harmine derivatives were designed, synthesized and evaluated as dual GSK-3β/DYRK1A inhibitors for their multiple biol. activities. The in vitro results indicated that most of them displayed promising activity against GSK-3β and DYRK1A. Among them, compound ZDWX-25 (I) showed potent inhibitory effects on GSK-3β and DYRK1A with IC50 values of 71 and 103 nM, resp. Mol. modeling and kinetic studies verified that ZDWX-25 could interact with the ATP binding pocket of GSK-3β and DYRK1A. Western blot anal. revealed that ZDWX-25 inhibited hyperphosphorylation of tau protein in okadaic acid (OKA)-induced SH-SY5Y cells. In addition, ZDWX-25 showed good blood-brain barrier penetrability in vitro. More importantly, ZDWX-25 could ameliorate the impaired learning and memory in APP/PS1/Tau transgenic mice. These results indicated that the harmine-based compounds could be served as promising dual-targeted candidates for AD. In the experiment, the researchers used Pyridin-3-ylboronic acid(cas: 1692-25-7HPLC of Formula: 1692-25-7)

Pyridin-3-ylboronic acid(cas: 1692-25-7) belongs to pyridine. Pyridines form stable salts with strong acids. Pyridine itself is often used to neutralize acid formed in a reaction and as a basic solvent. HPLC of Formula: 1692-25-7

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Mukherjee, Debojyoti; Manna, Rabindra Nath; Saha, Paramita; Mandal, Ujjwal; Mitra, Mainak published their research in Journal of Molecular Structure in 2021. The article was titled 《Electronic and molecular characterization of an air-stable Cr(II) complex containing azo-anion-radicals》.Recommanded Product: 141-86-6 The article contains the following contents:

A new mononuclear homoleptic chromium complex has been synthesized by reaction of one equivalent of Cr(CO)6 with two equivalent of the azoarom. pincer ligand namely 2,6-bis[(4-methylphenyl)azo]pyridine [LMe] in n-octane under reflux condition. The complex has been fully characterized by ESI-MS, 1H-NMR, FT-IR and UV/Vis spectroscopy. The X-ray structure of the complex reveals that the Cr-metal is coordinated to the central pyridine N-atom and two azo N-atoms of each tridentate pincer ligand in an octahedral environment. The 1H-NMR spectrum of the complex is indicative of diamagnetic ground state. The elongation of N-N bond lengths [d(N-N)av = 1.3275 Å] in the complex is consistent with the presence of azo-anion-radical character in the ligand. Since 2,6-bis(phenylazo)pyridine and its 4-Me-derivative are redox non-innocence in nature and therefore can coordinate to the chromium metal center as neutral (L0) or as mono-anionic mono-radical (L·)1- or as di-anionic di-radical (L··)2- or even as tri-anionic mono-radical (L·)3- resulting an ambiguity on the true oxidation state of the metal center. Thus the present work nicely elaborates the importance of suitably designed bis-azopyridine containing pincer ligand in accessing an air-stable Cr(II) complex starting with low-valent metal carbonyl precursor via electron transfer from the metal center to the highly π-acidic ligand leading to stable azo-anion-radicals. The stability of azo-anion-radical bound Cr(II) complex has been investigated by DFT calculations The experimental process involved the reaction of 2,6-Diaminopyridine(cas: 141-86-6Recommanded Product: 141-86-6)

2,6-Diaminopyridine(cas: 141-86-6) belongs to pyridine. Pyridine and its simple derivatives are stable and relatively unreactive liquids, with strong penetrating odours that are unpleasant.Recommanded Product: 141-86-6

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Dhau, Jaspreet S.; Singh, Avtar; Brandao, Paula; Felix, Vitor published their research in Inorganic Chemistry Communications in 2021. The article was titled 《Synthesis, characterization, X-ray crystal structure and antibacterial activity of bis[3-(4-chloro-N,N-diethylpyridine-2-carboxamide)] diselenide》.Formula: C6H5NO2 The article contains the following contents:

An efficient methodol. for the synthesis of bis[3-(4-chloro-N,N-diethylpyridine-2-carboxamide)] diselenide has been successfully achieved through ring lithiation using 2.2 equiv of lithium diisopropylamide (LDA) in THF. The hitherto unknown compound has been fully characterized by spectroscopic techniques NMR (1H and 13C), Mass spectrometry and elemental anal. The crystal structure of bis[3-(4-chloro-N,N-diethylpyridine-2-carboxamide)] diselenide has been determined by single crystal x-ray diffraction. The diselenide crystallizes in the monoclinic system (C2/c) with torsional angle of the selenium atoms attached to pyridyl rings (-C1-Se-Se-C1-) is -77.5(1). Bis[3-(4-chloro-N,N-diethylpyridine-2-carboxamide)] diselenide was found antibacterial active and results were compared with the most studied pyridylselenium compound (2,2′-dipyridyl diselenide) and standard drug Ampicillin. After reading the article, we found that the author used Picolinic acid(cas: 98-98-6Formula: C6H5NO2)

Picolinic acid(cas: 98-98-6) is used in the preparation of 2-Aminodihydro[1,3]thiazines as BACE 2 inhibitors and their preparation and use in the treatment of diabetes.Formula: C6H5NO2

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Bandarage, Upul K.; Aronov, Alex M.; Cao, Jingrong; Come, Jon H.; Cottrell, Kevin M.; Davies, Robert J.; Giroux, Simon; Jacobs, Marc; Mahajan, Sudipta; Messersmith, David; Moody, Cameron S.; Swett, Rebecca; Xu, Jinwang published their research in ACS Medicinal Chemistry Letters in 2021. The article was titled 《Discovery of a Novel Series of Potent and Selective Alkynylthiazole-Derived PI3Kγ Inhibitors》.Electric Literature of C7H5N The article contains the following contents:

Phosphoinositide 3-kinases (PI3Ks) are a family of enzymes that control a wide variety of cellular functions such as cell growth, proliferation, differentiation, motility, survival, and intracellular trafficking. PI3Kγ plays a critical role in mediating leukocyte chemotaxis as well as mast cell degranulation, making it a potentially interesting target for autoimmune and inflammatory diseases. We previously disclosed a novel series of PI3Kγ inhibitors derived from a benzothiazole core. The truncation of the benzothiazole core led to the discovery of a structurally diverse alkynyl thiazole series which displayed high PI3Kγ potency and subtype selectivity. Further medicinal chem. optimization of the alkynyl thiazole series led to identification of compounds such as 14 and 32, highly potent, subtype selective, and CNS penetrant PI3Kγ inhibitors. Compound 14 showed robust inhibition of PI3Kγ mediated neutrophil migration in vivo. In the part of experimental materials, we found many familiar compounds, such as 4-Ethynylpyridine(cas: 2510-22-7Electric Literature of C7H5N)

4-Ethynylpyridine(cas: 2510-22-7) belongs to pyridine. Pyridine is widely used in the precursor to agrochemicals and pharmaceuticals. Also, it is used as an important reagent and organic solvent.Electric Literature of C7H5N

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Favalli, Nicholas; Bassi, Gabriele; Bianchi, Davide; Scheuermann, Jorg; Neri, Dario published their research in Bioorganic & Medicinal Chemistry in 2021. The article was titled 《Large screening of DNA-compatible reaction conditions for Suzuki and Sonogashira cross-coupling reactions and for reverse amide bond formation》.HPLC of Formula: 2510-22-7 The article contains the following contents:

Progress in DNA-encoded chem. library synthesis and screening crucially relies on the availability of DNA-compatible reactions, which proceed with high yields and excellent purity for a large number of possible building blocks. In the past, exptl. conditions have been presented for the execution of Suzuki and Sonogashira cross-coupling reactions on-DNA. In this article, our aim was to optimize Suzuki and Sonogashira reactions, comparing our results to previously published procedures. We have tested the performance of improved conditions using 606 building blocks (including boronic acids, pinacol boranes and terminal alkynes), achieving >70% conversion for 84% of the tested mols. Moreover, we describe efficient exptl. conditions for the on-DNA synthesis of amide bonds, starting from DNA derivatives carrying a carboxylic acid moiety and 300 primary, secondary and aromatic amines, as amide bonds are frequently found in DNA-encoded chem. libraries thanks to their excellent DNA compatibility.4-Ethynylpyridine(cas: 2510-22-7HPLC of Formula: 2510-22-7) was used in this study.

4-Ethynylpyridine(cas: 2510-22-7) belongs to pyridine. Pyridine is widely used in the precursor to agrochemicals and pharmaceuticals. Also, it is used as an important reagent and organic solvent.HPLC of Formula: 2510-22-7

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

《Design, synthesis and anticancer properties of isocombretapyridines as potent colchicine binding site inhibitors》 was written by Shuai, Wen; Li, Xinnan; Li, Wenlong; Xu, Feijie; Lu, Lixue; Yao, Hong; Yang, Limei; Zhu, Huajian; Xu, Shengtao; Zhu, Zheying; Xu, Jinyi. HPLC of Formula: 1122-54-9 And the article was included in European Journal of Medicinal Chemistry in 2020. The article conveys some information:

A series of novel isocombretapyridines were designed and synthesized based on a lead compound isocombretastatin A-4 (isoCA-4) by replacing 3,4,5-trimethoxylphenyl with substituent pyridine nucleus. The MTT assay results showed that compound I possessed the most potent activities against all tested cell lines with IC50 values at nanomolar concentration ranges. Moreover, I inhibited tubulin polymerization at a micromolar level and also displayed potent anti-vascular activity in vitro. Further mechanistic studies were conducted to demonstrate that compound I could bind to the colchicine site of tubulin,and disrupte the cell microtubule networks, induce G2/M phase arrest, promote apoptosis and depolarize mitochondria of K562 cells in a dose-dependent manner. Notably, I exhibited more potent tumor growth inhibition activity with 68.7% tumor growth inhibition than that of isoCA-4 in H22 allograft mouse model without apparent toxicity. The present results suggested that compound I may serve as a promising potent microtubule-destabilizing agent candidate for the development of therapeutics to treat cancer. In the experiment, the researchers used 4-Acetylpyridine(cas: 1122-54-9HPLC of Formula: 1122-54-9)

4-Acetylpyridine(cas: 1122-54-9) belongs to pyridine. Pyridine is a relatively complex molecule and exhibits a number of different bands in IR spectra. Among others, the bands characterizing the ν8a and ν19b modes have been found to be sensitive to the coordination or protonation of the molecule. Note that the band that is diagnostic for the PyH+ ion at about 1545 cm− 1 (ν19b mode) does not overlap with any of the other bands.HPLC of Formula: 1122-54-9

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

In 2015,Kobayashi, Toshiki; Furusawa, Yuki; Yamada, Shoya; Akehi, Masaru; Takenaka, Fumiaki; Sasaki, Takanori; Akahoshi, Akiya; Hanada, Takahisa; Matsuura, Eiji; Hirano, Hiroyuki; Tai, Akihiro; Kakuta, Hiroki published 《Positron Emission Tomography to Elucidate Pharmacokinetic Differences of Regioisomeric Retinoid X Receptor Agonists》.ACS Medicinal Chemistry Letters published the findings.Safety of 5-Bromo-2-chloropyridine The information in the text is summarized as follows:

RXR partial agonist NEt-4IB (2a, 6-[ethyl-(4-isobutoxy-3-isopropylphenyl)amino]pyridine-3-carboxylic acid: EC50 = 169 nM, Emax = 55%) showed a blood concentration higher than its Emax after single oral administration at 30 mg/kg to mice, and repeated oral administration at 10 mg/kg/day to KK-Ay mice afforded antitype 2 diabetes activity without the side effects caused by RXR full agonists. However, RXR full agonist NEt-3IB (1a), in which the isobutoxy and iso-Pr groups of 2a are interchanged, gave a much lower blood concentration than 2a. Here we used positron emission tomog. (PET) with tracers [11C]1a, [11C]2a and fluorinated derivatives [18F]1b, [18F]2b, which have longer half-lives, to examine the reason why 1a and 2a exhibited significantly different blood concentrations As a result, the reason for the high blood concentration of 2a after oral administration was found to be linked to higher intestinal absorbability together with lower biliary excretion, compared with 1a. The experimental part of the paper was very detailed, including the reaction process of 5-Bromo-2-chloropyridine(cas: 53939-30-3Safety of 5-Bromo-2-chloropyridine)

5-Bromo-2-chloropyridine(cas: 53939-30-3) belongs to pyridine. Pyridine derivatives lend themselves to many roles in the spirited field of supramolecular chemistry – whether as the ligand backbone of metal-organic polymers or presiding over the key electronic stations of nanodevices. In biochemistry, pyridine-containing cofactors are necessary nutrients on which our lives depend. Safety of 5-Bromo-2-chloropyridine

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem