Day: November 8, 2022

The author of 《A Biased Agonist at Immunometabolic Receptor GPR84 Causes Distinct Functional Effects in Macrophages》 were Lucy, Daniel; Purvis, Gareth S. D.; Zeboudj, Lynda; Chatzopoulou, Maria; Recio, Carlota; Bataille, Carole J. R.; Wynne, Graham M.; Greaves, David R.; Russell, Angela J.. And the article was published in ACS Chemical Biology in 2019. Related Products of 103-74-2 The author mentioned the following in the article:

GPR84 is an orphan G-protein-coupled receptor that is expressed on immune cells and implicated in several inflammatory diseases. The validation of GPR84 as a therapeutic target is hindered by the narrow range of available chem. tools and consequent poor understanding of GPR84 pathophysiol. Here we describe the discovery and characterization of DL-175, a potent, selective, and structurally novel GPR84 agonist and the first to display significantly biased signaling across GPR84-overexpressing cells, primary murine macrophages, and human U937 cells. By comparing DL-175 with reported GPR84 ligands, we show for the first time that biased GPR84 agonists have markedly different abilities to induce chemotaxis in human myeloid cells, while causing similar levels of phagocytosis enhancement. This work demonstrates that biased agonism at GPR84 enables the selective activation of functional responses in immune cells and delivers a high-quality chem. probe for further investigation. In the part of experimental materials, we found many familiar compounds, such as 2-(2-Hydroxyethyl)pyridine(cas: 103-74-2Related Products of 103-74-2)

2-(2-Hydroxyethyl)pyridine(cas: 103-74-2) 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. Related Products of 103-74-2

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

The author of 《Mitochondrion-targeted two-photon probes: Real-time monitoring endogenous GSH via situ reaction in Hela cells》 were Zhang, Huihui; Zhang, Gaojian; Liu, Gang; Xia, Ying; Fang, Min; Zhu, Xiaojiao; Wu, Zhichao; Li, Xiaowu; Yang, Xingyuan; Zhou, Hongping. And the article was published in Dyes and Pigments in 2019. Application In Synthesis of 2-(Bromomethyl)pyridine hydrobromide The author mentioned the following in the article:

Mitochondria and glutathione (GSH) play crucial roles in human pathologies. To better understand the disease mechanisms, two-photon fluorescence probes responding to mitochondria and glutathione were urgently pursued. Here, a series of two-photon fluorescence probes (5a, 5b and 5c) were prepared, which could detect GSH as well as target mitochondria. The probes delivered high and rapid selectivity towards GSH among the various biothiols and qual. monitored the endogenous cellular GSH in real-time via a two-photon laser confocal fluorescence microscopy. Furthermore, the theor. understanding of high selectivity in two-photon fluorescence probes were also performed. The combined results demonstrated that the probes would function as efficient tools in bio-imaging and biol. diagnosis. The experimental part of the paper was very detailed, including the reaction process of 2-(Bromomethyl)pyridine hydrobromide(cas: 31106-82-8Application In Synthesis of 2-(Bromomethyl)pyridine hydrobromide)

2-(Bromomethyl)pyridine hydrobromide(cas: 31106-82-8) 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.Application In Synthesis of 2-(Bromomethyl)pyridine hydrobromide

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

The author of 《Regulation of Substituent Effects on Configurations and Magnetic Performances of Mononuclear DyIII Single-Molecule Magnets》 were Zhang, Sheng; Mo, Wenjiao; Zhang, Jiangwei; Zhang, Zengqi; Yin, Bing; Hu, Dengwei; Chen, Sanping. And the article was published in Inorganic Chemistry in 2019. COA of Formula: C12H12N2 The author mentioned the following in the article:

A series of mononuclear DyIII compounds, [Dy(tmpd)3(4,4′-dmpy)] (1), [Dy(tffb)3(4,4′-dmpy)] (2), [Dy(tffb)3(5,5′-dmpy)] (3), and [Dy(tmpd)3(5,5′-dmpy)] () [tmpd = 4,4,4-trifluoro-1-(4-methoxyphenyl)-1,3-butanedione, tffb = 4,4,4-trifluoro-1-(4-fluorophenyl)-1,3-butanedione, 4,4′-dmpy = 4,4′-dimethyl-2,2′-bipyridyl, and 5,5′-dmpy = 5,5′-dimethyl-2,2′-bipyridyl], have been synthesized by modifying β-diketonate ligands and capping N-donor co-ligands. DyIII ions in 1-4 possess N2O6 octacoordinated environments. Compounds 1 and 2 exhibit distorted trigonal dodecahedron configurations, while 3 and 4 display distorted square antiprismatic configurations. Systematic investigations of the a.c. measurements indicate the different magnetic relaxation dynamics with energy barriers (Ueff) of 66 K (1, 45 cm-1), 189 K, (2, 131 cm-1), 115 K (3, 79 cm-1), and 205 K (4, 142 cm-1). To deeply understand their different magnetic behaviors, the magnetic anisotropies of 1-4 were studied by ab initio calculations From ab initio calculations, the energies of the first excited state (KD1) are consistent with the exptl. Ueff under zero d.c. field. Compound 4 presents the largest Ueff because of the smallest gX,Y and μqTM as well as the most strong axial crystal field parameters (CFPs) among compounds 1-4. The M vs. H data exhibit butterfly-shaped hysteresis loops at 2 K for 1-4. The different coordination geometries, the magnetic dynamics, the electrostatic repulsion, and CFPs result from the different substituent effects of ligands, including the electronic effect, the steric effect, and the positions of substituted groups. The different coordination geometries, the magnetic dynamics, the electrostatic repulsion, and the crystal field parameters result from the different substituent effects of ligands, including the electronic effect, the steric effect, and the positions of substituted groups. After reading the article, we found that the author used 4,4′-Dimethyl-2,2′-bipyridine(cas: 1134-35-6COA of Formula: C12H12N2)

4,4′-Dimethyl-2,2′-bipyridine(cas: 1134-35-6) is used as a chemical Intermediate. It can be used for the determination of ferrous and cyanide compounds.COA of Formula: C12H12N2 Furthermore, 4,4′-Dimethyl-2,2′-bipyridine is used in the synthesis of a series of o-phenanthroline-substituted ruthenium(II) complexes.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

The author of 《Selective C-C bond formation from rhodium-catalyzed C-H activation reaction of 2-arylpyridines with 3-aryl-2H-azirines》 were Baek, Yonghyeon; Kim, Jinwoo; Hyunseok Kim; Jung, Seung Jin; Ryu, Ho; Kim, Suyeon; Son, Jeong-Yu; Um, Kyusik; Han, Sang Hoon; Seo, Hyung Jin; Heo, Juyoung; Lee, Kooyeon; Baik, Mu-Hyun; Lee, Phil Ho. And the article was published in Chemical Science in 2019. Formula: C6H6BrN The author mentioned the following in the article:

A novel method for the synthesis of acylmethyl-substituted 2-arylpyridine derivatives I [R1 = Ph, 4-MeC6H4, 2-ClC6H4, etc.; R2 = 4-Me, 5-C(O)Me, 5-CF3, etc.; R3 = H, Me, F, C(O)Me, CO2Et] was synthesized via rhodium-catalyzed C-H activation reaction of 3-aryl-2H-azirines with 2-arylpyridines and explored a prototype reaction using DFT-calculations Computational studies quickly revealed and prototype exptl. work confirmed that neither the formation of the expected metal nitrene complexes nor the C-N coupling were viable. Instead, azirine ring-opening followed by C-C coupling was found to be much more favorable to give imines that readily underwent hydrolysis in aqueous conditions to form compounds I. This new method was highly versatile and selective toward a wide range of substrates with high functional group tolerance. The results came from multiple reactions, including the reaction of 2-Bromo-5-methylpyridine(cas: 3510-66-5Formula: C6H6BrN)

2-Bromo-5-methylpyridine(cas: 3510-66-5) 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. Formula: C6H6BrN

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

《Tuned Al3+ selectivity and π-extended properties of di-2-picolylamine-substituted quinoline-based tolan》 was published in Tetrahedron Letters in 2020. These research results belong to Ko, Min-Sung; Kurapati, Sathish; Jo, Yunhee; Cho, Beomhee; Cho, Dong-Gyu. Name: Bis(pyridin-2-ylmethyl)amine The article mentions the following:

Di-2-picolylamine (DPA)-substituted quinoline-type tolan was synthesized herein. The electron withdrawing CN substituted tolan (1)(I) exhibited clear Al3+ selectivity, unlike simple DPA-substituted quinoline (2). Addnl., owing to the π-extension to quinoline (2), a red shifted fluorescence band and the shoulder of tolan (1) were observed at 491 and 537 nm, resp., whereas the quinoline (2) fluorescence band was observed at approx. 450 nm. Consequently, Al3+ bound tolan was more red shifted in comparison with other metal ions bound by 2. Fluorescence titration of Al3+ to 1 (20μM) in HEPES buffer (10 mM, pH = 7.4) containing 50% MeOH exhibited a limit of detection of 36 nM. The results came from multiple reactions, including the reaction of Bis(pyridin-2-ylmethyl)amine(cas: 1539-42-0Name: Bis(pyridin-2-ylmethyl)amine)

Bis(pyridin-2-ylmethyl)amine(cas: 1539-42-0) is a secondary amine with two picolyl substituents. As a tridentate ligand this compound provides three nitrogen donors that affords good selectivity for Zn2+ over biologically relevant metals such as Na+, K+, Mg2+ and Ca2+, and leaves coordination sites free for anion binding. Name: Bis(pyridin-2-ylmethyl)amine

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

《Chromium picolinate attenuates cognitive deficit in ICV-STZ rat paradigm of sporadic Alzheimer’s-like dementia via targeting neuroinflammatory and IRS-1/PI3K/AKT/GSK-3β pathway》 was published in Inflammopharmacology in 2020. These research results belong to Akhtar, Ansab; Dhaliwal, Jatinder; Saroj, Priyanka; Uniyal, Ankit; Bishnoi, Mahendra; Sah, Sangeeta Pilkhwal. COA of Formula: C6H5NO2 The article mentions the following:

Alzheimer’s disease (AD) is prevalent in old age people and is one of the most common brain diseases. Brain insulin resistance, neuroinflammation, oxidative stress, and mitochondrial and cholinergic dysfunction are key features of the disease. In our study, streptozotocin (STZ) in a dose of 3 mg/kg was injected in male Wistar rats bilaterally through the intracerebroventricular (ICV) route on stereotaxic apparatus Chromium picolinate (CrPic) was tested at doses of 1 mg/kg, 2 mg/kg, and 4 mg/kg, while rivastigmine (2 mg/kg) was used as reference standard drug. Cognitive dysfunction induced by STZ was assessed by behavioral tests like Morris water maze and novel object recognition test. Treatment with CrPic revealed attenuation of cognitive deficit. STZ-induced neuroinflammation evident by increased TNF-α, IL-6, and CRP levels was also significantly decreased by CrPic. Dysfunctional insulin signaling after ICV-STZ was demonstrated by reduced IRS-1, PI3K, AKT, BDNF gene expression, and increased GSK-3β, NF-κB gene expression with the help of qRT-PCR. CrPic treatment produced an improvement in insulin signaling revealed by increased gene expression of IRS-1, PI3-K, AKT, BDNF, and decreased gene expression of GSK-3β and NF-κB. It was concluded that CrPic reversed AD pathol. revealed by improved memory, reduced oxidative stress, neuroinflammation, mitochondrial dysfunction, and upregulated insulin signaling. The experimental process involved the reaction of Picolinic acid(cas: 98-98-6COA of Formula: 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.COA of Formula: C6H5NO2

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

《Enantiopure substituted pyridines as promising antimalarial drug candidates》 was published in Tetrahedron in 2020. These research results belong to Bentzinger, Guillaume; Pair, Etienne; Guillon, Jean; Marchivie, Mathieu; Mullie, Catherine; Agnamey, Patrice; Dassonville-Klimpt, Alexandra; Sonnet, Pascal. Formula: C5H3Br2N The article mentions the following:

The enantioselective synthesis and biol. evaluation of 4-(2-amino-1-hydroxyethyl)pyridines I [R1 = n-Bu, n-pentyl, n-hexyl, n-heptyl] as new antimalarial drug candidates was described. In particular, two routes to obtain the key-intermediate 4-vinyl-pyridine were studied. These routes were based on a Krohnke-type cyclization or on metal-catalyzed reactions. The Krohnke-type cyclization route was faster but only efficient at low scale since this pathway involved a Wittig reaction that requires severe temperature-control. Consequently, we designed a second route based on metal-catalyzed reactions. This way was longer but the 4-vinyl-pyridine could be obtained on a 5 g scale at least. Finally, a regioselective SN2 ring-opening of enantiopure epoxides by alkyl primary amines allowed the synthesis of eight I with global yields up to 41%. These compounds showed strong in vitro antimalarial activity against P. falciparum strains and were more active that chloroquine and mefloquine. These results demonstrated that I were promising antimalarial drug candidates. In the experimental materials used by the author, we found 2,6-Dibromopyridine(cas: 626-05-1Formula: C5H3Br2N)

2,6-Dibromopyridine(cas: 626-05-1) 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.Formula: C5H3Br2N

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

《ESI-MS Study of the Interaction of Potential Oxidovanadium(IV) Drugs and Amavadin with Model Proteins》 was published in Inorganic Chemistry in 2020. These research results belong to Ugone, Valeria; Sanna, Daniele; Sciortino, Giuseppe; Crans, Debbie C.; Garribba, Eugenio. Synthetic Route of C6H5NO2 The article mentions the following:

In this study, the binding to lysozyme (Lyz) of four important VIV compounds with antidiabetic and/or anticancer activity, [VIVO(pic)2(H2O)], [VIVO(ma)2], [VIVO(dhp)2], and [VIVO(acac)2], where pic-, ma-, dhp-, and acac- are picolinate, maltolate, 1,2-dimethyl-3-hydroxy-4(1H)-pyridinonate, and acetylacetonate anions, and of the vanadium-containing natural product amavadin ([VIV(hidpa)2]2-, with hidpa3-N-hydroxyimino-2,2′-diisopropionate) was investigated by ElectroSpray Ionization-Mass Spectrometry (ESI-MS). Moreover, the interaction of [VIVO(pic)2(H2O)], chosen as a representative VIVO2+ complex, was examined with two addnl. proteins, myoglobin (Mb) and ubiquitin (Ub), to compare the data. The examined vanadium concentration was in the range 15-150 μM, i.e., very close to that found under physiol. conditions. With pic-, dhp-, and hidpa3-, the formation of adducts n[VIVOL2]-Lyz or n[VIVL2]-Lyz is favored, while with ma- and acac- the species n[VIVOL]-Lyz are detected, with n dependent on the exptl. VIV/protein ratio. The behavior of the systems with [VIVO(pic)2(H2O)] and Mb or Ub is very similar to that of Lyz. The results suggested that under physiol. conditions, the moiety cis-VIVOL2 (L = pic-, dhp-) is bound by only one accessible side-chain protein residue that can be Asp, Glu, or His, while VIVOL+ (L = ma-, acac-) can interact with the two equatorial and axial sites. If the VIV complex is thermodynamically stable and does not have available coordination positions, such as amavadin, the protein cannot interact with it through the formation of coordination bonds and, in such cases, noncovalent interactions are predicted. The formation of the adducts is dependent on the thermodn. stability and geometry in aqueous solution of the VIVO2+ complex and affects the transport, uptake, and mechanism of action of potential V drugs. The potentiality of ElectroSpray Ionization-Mass Spectrometry (ESI-MS) to determine the number and composition of adducts formed by labile V complexes with potential pharmacol. application and the natural product amavadin with some proteins was examined ESI-MS allows the study of vanadium concentrations close to those found under physiol. conditions. The nature of the adducts-which could be related to the transport, uptake, and mechanism of action of potential V drugs-depends on the structure and thermodn. stability at concentrations around micromolar. In the experiment, the researchers used Picolinic acid(cas: 98-98-6Synthetic Route of 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.Synthetic Route of C6H5NO2

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

《Bis(zinc(II)-dipicolylamine)-functionalized sub-2 μm core-shell microspheres for the analysis of N-phosphoproteome》 was published in Nature Communications in 2020. These research results belong to Hu, Yechen; Jiang, Bo; Weng, Yejing; Sui, Zhigang; Zhao, Baofeng; Chen, Yuanbo; Liu, Lukuan; Wu, Qiong; Liang, Zhen; Zhang, Lihua; Zhang, Yukui. Product Details of 1539-42-0 The article mentions the following:

Protein N-phosphorylation plays a critical role in central metabolism and two/multicomponent signaling of prokaryotes. However, the current enrichment methods for O-phosphopeptides are not preferred for N-phosphopeptides due to the intrinsic lability of P-N bond under acidic conditions. Therefore, the effective N-phosphoproteome anal. remains challenging. Herein, bis(zinc(II)-dipicolylamine)-functionalized sub-2 μm core-shell silica microspheres (SiO2@DpaZn) are tailored for rapid and effective N-phosphopeptides enrichment. Due to the coordination of phosphate groups to Zn(II), N-phosphopeptides can be effectively captured under neutral conditions. Moreover, the method is successfully applied to an E.coli and HeLa N-phosphoproteome study. These results further broaden the range of methods for the discovery of N-phosphoproteins with significant biol. functions. In the experiment, the researchers used many compounds, for example, Bis(pyridin-2-ylmethyl)amine(cas: 1539-42-0Product Details of 1539-42-0)

Bis(pyridin-2-ylmethyl)amine(cas: 1539-42-0) is a secondary amine with two picolyl substituents. As a tridentate ligand this compound provides three nitrogen donors that affords good selectivity for Zn2+ over biologically relevant metals such as Na+, K+, Mg2+ and Ca2+, and leaves coordination sites free for anion binding. Product Details of 1539-42-0

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

《Redox cycling of copper by coumarin-di(2-picolyl)amine hybrid molecule leads to ROS-mediated modulation of redox scavengers, DNA damage and cell death in diethylnitrosamine induced hepatocellular carcinoma》 was published in Bioorganic Chemistry in 2020. These research results belong to Khan, Saman; Zafar, Atif; Naseem, Imrana. Product Details of 1539-42-0 The article mentions the following:

Targeted therapy is a new strategy for cancer treatment that targets chem. entities specific to cancer cells than normal ones. One of the features associated with malignancy is the elevated copper which plays an integral role in angiogenesis. Work is in progress in our lab to identify new copper chelators to target elevated copper under targeted therapy for the killing of cancer cells. Recently, a coumarin-based copper chelator, di(2-picolyl)amine-3(bromoacetyl)coumarin hybrid mol. (ligand-L) has been synthesized by us, and also studied its copper-dependent macromol. damage response in copper overloaded lymphocytes. The present study investigates the anticancer activity of ligand-L and its mode of action in rat model of diethylnitrosamine (DEN) induced hepatocellular carcinoma. It has been found that liver tissue has a marked increase in copper levels in DEN induced hepatocellular carcinoma. Ex vivo results showed that ligand-L inhibited cell viability, induced reactive oxygen species (ROS) generation, DNA damage, loss of mitochondrial membrane potential and caspase-3 activation in isolated hepatocellular carcinoma cells (HCC). All these effects induced by ligand-L were abrogated by neocuproine and N-acetylcysteine (ROS scavenger). Further, ligand-L treatment of animals bearing hepatocellular carcinoma results in an increment in the cellular redox scavengers, lipid peroxidation and DNA breakage in malignant hepatocytes. In vivo studies using ligand-L also showed that ligand-L possesses anticancer properties as evidenced by improvement in liver marker enzymes and liver surface morphol., and reduced alpha-fetoprotein in the treated group compared to untreated cancer-induced group. Overall, this study suggests that copper-ligand-L interaction leads to ROS generation which caused DNA damage and apoptosis in malignant cells. This study provides enough support to establish ligand-L as a clin. relevant lead mol. for the treatment of different malignancies. In the experiment, the researchers used many compounds, for example, Bis(pyridin-2-ylmethyl)amine(cas: 1539-42-0Product Details of 1539-42-0)

Bis(pyridin-2-ylmethyl)amine(cas: 1539-42-0) is a secondary amine with two picolyl substituents. As a tridentate ligand this compound provides three nitrogen donors that affords good selectivity for Zn2+ over biologically relevant metals such as Na+, K+, Mg2+ and Ca2+, and leaves coordination sites free for anion binding. Product Details of 1539-42-0

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem