Pyridine-derivatives

Katsuya, Ken; Oikawa, Daisuke; Iio, Kiyosei; Obika, Shingo; Hori, Yuji; Urashima, Toshiki; Ayukawa, Kumiko; Tokunaga, Fuminori published the artcile< Small-molecule inhibitors of linear ubiquitin chain assembly complex (LUBAC), HOIPINs, suppress NF-kB signaling>, Synthetic Route of 329214-79-1, the main research area is LUBAC HOIPIN nuclear factor signalling; Cytokine; Enzyme inhibitor; Inflammation; NF-κB; Ubiquitin.

Nuclear factor-kB (NF-kB) is a crucial transcription factor family involved in the regulation of immune and inflammatory responses and cell survival. The linear ubiquitin chain assembly complex (LUBAC), composed of the HOIL-1L, HOIP, and SHARPIN subunits, specifically generates Met1-linked linear ubiquitin chains through the ubiquitin ligase activity in HOIP, and activates the NF-kB pathway. We recently identified a chem. inhibitor of LUBAC, which we named HOIPIN-1 (HOIP inhibitor-1). To improve the potency of HOIPIN-1, we synthesized 7 derivatives (HOIPIN-2~8), and analyzed their effects on LUBAC and NF-kB activation. Among them, HOIPIN-8 suppressed the linear ubiquitination activity by recombinant LUBAC at an IC50 value of 11 nM, corresponding to a 255-fold increase over that of HOIPIN-1. Furthermore, as compared with HOIPIN-1, HOIPIN-8 showed 10-fold and 4-fold enhanced inhibitory activities on LUBAC- and TNF-a-induced NF-kB activation resp., without cytotoxicity. These results indicated that HOIPIN-8 is a powerful tool to explore the physiol. functions of LUBAC.

Biochemical and Biophysical Research Communications published new progress about Animal gene, ICAM1 Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 329214-79-1 belongs to class pyridine-derivatives, and the molecular formula is C11H16BNO2, Synthetic Route of 329214-79-1.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Xie, Qiqiang; Dong, Guangbin published the artcile< Programmable Ether Synthesis Enabled by Oxa-Matteson Reaction>, Formula: C11H16BNO2, the main research area is boronate alkyl aryl oxa Matteson oxygen carbenoid insertion reaction; boron substituted ether product preparation.

The Matteson-type reactions have received increasing interest in constructing complex organic mols. via iterative synthetic strategies; however, the current tactics are almost exclusively based on homologation of pure C chains. Here, the authors report the development of the oxa-Matteson reaction that enables sequential O and carbenoid insertions into diverse alkyl- and arylboronates. It offers a distinct entry to a wide range of B-substituted ethers. The utilities of this method are demonstrated in the preparation of various functional ethers, the asym. synthesis of an acetyl-CoA-carboxylase inhibitor, and the programmable construction of polyethers.

Journal of the American Chemical Society published new progress about Boronic acids, esters Role: RCT (Reactant), RACT (Reactant or Reagent) (alkyl and aryl). 329214-79-1 belongs to class pyridine-derivatives, and the molecular formula is C11H16BNO2, Formula: C11H16BNO2.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Gardell, Stephen J.; Hopf, Meghan; Khan, Asima; Dispagna, Mauro; Hampton Sessions, E.; Falter, Rebecca; Kapoor, Nidhi; Brooks, Jeanne; Culver, Jeffrey; Petucci, Chris; Ma, Chen-Ting; Cohen, Steven E.; Tanaka, Jun; Burgos, Emmanuel S.; Hirschi, Jennifer S.; Smith, Steven R.; Sergienko, Eduard; Pinkerton, Anthony B. published the artcile< Boosting NAD+ with a small molecule that activates NAMPT>, Formula: C6H8N2, the main research area is lung carcinoma cell NAMPT SBI797812 NAD.

Pharmacol. strategies that boost intracellular NAD+ are highly coveted for their therapeutic potential. One approach is activation of nicotinamide phosphoribosyltransferase (NAMPT) to increase production of NMN (NMN), the predominant NAD+ precursor in mammalian cells. A high-throughput screen for NAMPT activators and hit-to-lead campaign yielded SBI-797812, a compound that is structurally similar to active-site directed NAMPT inhibitors and blocks binding of these inhibitors to NAMPT. SBI-797812 shifts the NAMPT reaction equilibrium towards NMN formation, increases NAMPT affinity for ATP, stabilizes phosphorylated NAMPT at His247, promotes consumption of the pyrophosphate byproduct, and blunts feedback inhibition by NAD+. These effects of SBI-797812 turn NAMPT into a “”super catalyst”” that more efficiently generates NMN. Treatment of cultured cells with SBI-797812 increases intracellular NMN and NAD+. Dosing of mice with SBI-797812 elevates liver NAD+. Small mol. NAMPT activators such as SBI-797812 are a pioneering approach to raise intracellular NAD+ and realize its associated salutary effects.

Nature Communications published new progress about Biomarkers. 3731-53-1 belongs to class pyridine-derivatives, and the molecular formula is C6H8N2, Formula: C6H8N2.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Rani, Pooja; Gauri; Husain, Ahmad; Bhasin, K. K.; Kumar, Girijesh published the artcile< A Doubly Interpenetrated CuII Metal-Organic Framework for Selective Molecular Recognition of Nitroaromatics>, COA of Formula: C6H8N2, the main research area is copper pyridinylnaphthalenecarboxamide oxybisbenzoate MOF preparation thermal stability fluorescent sensor; crystal structure copper pyridinylnaphthalenecarboxamide oxybisbenzoate MOF.

Herein, we report the design, synthesis, and structural characterization of a novel 2-fold interpenetrated CuII metal-organic framework Cu-MOF-1 [{Cu2(L)(oba)2}·DMF·H2O]α (where, L = N2,N6-di(pyridin-4-yl)naphthalene-2,6-dicarboxamide and oba2- is 4,41-oxybis(benzoic acid) anion). A single-crystal X-ray anal. reveals that Cu-MOF-1 exhibits a doubly (1 + 1) interpenetrated three-dimensional structure with 6-connected mab topol. Moreover, Cu-MOF-1 showed high fluorescence stability in methanol solution and selectively detected nitroaroms. with high quenching constants and low detection limits of 0.31 × 105 M-1 and 22.65μM for 2,4,6-TNP; 1.34 × 105 M-1 and 18.7μM for 4-NPH; and 1.49 × 105 M-1 and 14.07μM for 4-NA. Notably, ligand L itself did not display any type of recognition for any nitroaroms. in methanol solution The sensing of NACs by Cu-MOF-1 followed mostly the resonance energy transfer mechanism; however, in the case of 4-NPH and 2,4,6-TNP an electron transfer mechanism also exists. Importantly, Cu-MOF-1 shows recyclability up to five cycles without any significant loss in quenching efficiency.

Crystal Growth & Design published new progress about Aromatic nitro compounds Role: ANT (Analyte), ANST (Analytical Study). 3731-53-1 belongs to class pyridine-derivatives, and the molecular formula is C6H8N2, COA of Formula: C6H8N2.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Khatouri, M.; Lemaalem, M.; Ahfir, R.; El Khaoui, S.; Derouiche, A.; Filali, M. published the artcile< Sol/gel transition of oil/water microemulsions controlled by surface grafted triblock copolymer dodecyl-PEO227-dodecyl: molecular dynamics simulations with experimentally validated interaction potential>, Synthetic Route of 123-03-5, the main research area is soluble gel transition microemulsion copolymer mol dynamic simulation.

We studied a large range of identical spherical oil/water microemulsion (O/W-MI) volume fractions. The O/W-MIs are stabilized by cetylpyridinium chloride ionic surfactant (CpCl) and octanol cosurfactant and dispersed in salt water. We grafted different numbers of dodecyl-(polyEthylene oxide)227-dodecyl triblock copolymer that we note (n(D-PEO227-D)), where n varies from 0 to 12. We accomplished the grafting process by replacing a small amount of CpCl and octanol with the appropriate n(D-PEO227-D). The aim is to determine the interaction/structure relationship of the covered microemulsions. Precisely, we are interested in a quant. investigation of the influence of volume fraction Φ, temperature (T), and n(D-PEO227-D) on the microemulsion sol/gel transition. To this end, we first study the uncoated microemulsion structure depending only on Φ. Second, we determine the coated microemulsions structure as a function of n(D-PEO227-D) for different Φ. Third, we examine the effect of temperature on the uncoated and coated microemulsion. We show that the sol/gel transition is controlled by the three main parameters, Φ, T, and n(D-PEO227-D). Accordingly, the uncoated microemulsion sol/gel transition, at ambient temperature, occurred for Φ ≃ 33.65%. By increasing Φ, the O/W-MIs show a glass state, which occurs, along with the gel state, at Φ ≃ 37% and arises clearly at Φ ≃ 60%. The coated O/W-MI sol/gel transition is found to be linearly dependent on n(D-PEO227-D) and takes place for Φ ≃ 26.5% for n(D-PEO227-D) = 12. Ordinarily, the decrease in temperature leads to gel formation of microemulsions for low Φ. Addnl., in this work, we found that the gelation temperature increases linearly with n(D-PEO227-D). Thus, the parameter n(D-PEO227-D) can control the sol/gel transition of the O/W-MIs at ambient temperature and moderate Φ.

RSC Advances published new progress about Clusters. 123-03-5 belongs to class pyridine-derivatives, and the molecular formula is C21H38ClN, Synthetic Route of 123-03-5.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Wang, Runbin; Wei, Ming; Wang, Xuerong; Chen, Yushou; Xiong, Yanshi; Cheng, Jianxin; Tan, Yanhui; Liao, Xiangwen; Wang, Jintao published the artcile< Synthesis of ruthenium polypyridine complexes with benzyloxyl groups and their antibacterial activities against Staphylococcus aureus>, COA of Formula: C10H8N2, the main research area is Antibacterial activity; Antibacterial adjuvants; Biofilm; Membrane disruption; Ruthenium complex; Synergistic effect.

Four new ruthenium polypyridyl complexes, [Ru(bpy)2(BPIP)](PF6)2 (Ru(II)-1), [Ru(dtb)2(BPIP)](PF6)2 (Ru(II)-2), [Ru(dmb)2(BPIP)](PF6)2 (Ru(II)-3) and [Ru(dmob)2(BPIP)](PF6)2 (Ru(II)-4) (bpy = 2,2′-bipyridine, dtb = 4,4′-di-tert-butyl-2,2′-bipyridine, dmb = 4,4′-dimethyl-2,2′-bipyridine, dmob = 4,4′-dimethoxy-2,2′-bipyridine and BPIP = 2-(3,5-bis(benzyloxyl)phenyl)-1H-imidazo[4,5-f][1,10]phenanthroline) had been synthesized and characterized. Their antimicrobial activities were investigated against Staphylococcus aureus (S. aureus) and four complexes showed obvious antibacterial effect, especially the min. inhibition concentration (MIC) value of Ru(II)-3 was only 4 μg/mL. In addition, Ru(II)-3 was able to kill bacteria quickly and inhibit the formation of biofilm. Meanwhile, the cooperative effect between Ru(II)-3 and general antibiotics were tested and the results showed that Ru(II)-3 could enhance the susceptibility of S. aureus to different types of antibiotics. Most importantly, Ru(II)-3 hardly showed cytotoxicity to mammalian erythrocytes both in homelysis experiment and G. mellonella model. After being injected with high doses of the Ru(II)-3in vivo, the G. mellonella worms still exhibited high survival rates. Finally, a mouse skin infection model and G. mellonella infection model was built to determine the antibacterial activity of Ru(II)-3in vivo. The antibacterial mechanism of Ru(II)-3 was probably related to the membrane-disruption. Taken together, ruthenium polypyridine complexes with benzyloxyl groups had the potential to develop an attractive and untraditional antibacterial agent with new mode of action.

Journal of Inorganic Biochemistry published new progress about 366-18-7. 366-18-7 belongs to class pyridine-derivatives, and the molecular formula is C10H8N2, COA of Formula: C10H8N2.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Zhang, Xue; Wang, Yun; Li, Xiaoqing; Dai, Yejia; Wang, Qinghao; Wang, Guoyou; Liu, Depeng; Gu, Xuezhu; Yu, Dingrong; Ma, Yinlian; Zhang, Cun published the artcile< Treatment mechanism of Gardeniae fructus and its carbonized product against ethanol-induced gastric lesions in rats>, Reference of 93-60-7, the main research area is Gardeniae gastric lesions gastroprotective; Gardeniae Fructus; carbonized Gardeniae Fructus; ethanol-induced gastric lesion; gastroprotective; metabolomics; processed.

Gardeniae Fructus (GF) and carbonized GF (GFC) have been shown to exert a gastrointestinal protective effect and are frequently used in clin. practice for the treatment of hemorrhage and brown stool. In this study, we employed a combination of pharmacol. methods and metabolomics in a rat model of ethanol-induced acute stomach ulcer to investigate the gastroprotective effect of GF and GFC water extracts and the potential mechanism involved in this process. The levels of nitric oxide (NO) and interleukin 6 (IL-6) in the plasma of rats were determined The results showed that both GF and GFC reduced the ethanol-induced gastric lesions and expression of NO and IL-6 in these rats. Of note, 16 and 11 feature metabolites were filtered and identified in the GF and GFC groups, resp. Both GF and GFC act by restoring the biosynthesis of valine, leucine, and isoleucine, and the metabolism of glycerophospholipids. Moreover, histol. evaluation revealed that heat processing of GF to create GFC enhanced the gastric mucosa protective effect. Furthermore, heat processing converted the main pathway from alanine, aspartate, and glutamate metabolism, associated with GF, to histidine metabolism, associated with GFC. GF and GFC ameliorated gastric mucosa lesions in rats via reductions in NO production and inflammatory cytokine secretion, and the induction of prostaglandin E2.

Frontiers in Pharmacology published new progress about Biomarkers. 93-60-7 belongs to class pyridine-derivatives, and the molecular formula is C7H7NO2, Reference of 93-60-7.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Skepper, Colin K.; Moreau, Robert J.; Appleton, Brent A.; Benton, Bret M.; Drumm, Joseph E.; Feng, Brian Y.; Geng, Mei; Hu, Cheng; Li, Cindy; Lingel, Andreas; Lu, Yipin; Mamo, Mulugeta; Mergo, Wosenu; Mostafavi, Mina; Rath, Christopher M.; Steffek, Micah; Takeoka, Kenneth T.; Uehara, Kyoko; Wang, Lisha; Wei, Jun-Rong; Xie, Lili; Xu, Wenjian; Zhang, Qiong; de Vicente, Javier published the artcile< Discovery and Optimization of Phosphopantetheine Adenylyltransferase Inhibitors with Gram-Negative Antibacterial Activity>, Category: pyridine-derivatives, the main research area is triazolopyrimidinone azabenzimidazole preparation phosphopantetheine adenylyltransferase inhibitor antibacteria Escherichia.

In the preceding manuscript the authors described a successful fragment-based lead discovery (FBLD) strategy for discovery of bacterial phosphopantetheine adenylyltransferase inhibitors (PPAT, CoaD). Following several rounds of optimization two promising lead compounds were identified: triazolopyrimidinone (I) and 4-azabenzimidazole (II). Here the authors disclose the efforts to further optimize these two leads for on-target potency and Gram-neg. cellular activity. Enabled by a robust x-ray crystallog. system, the authors’ structure-based inhibitor design approach delivered compounds with biochem. potencies 4-5 orders of magnitude greater than their resp. fragment starting points. Addnl. optimization was guided by observations on bacterial permeability and physicochem. properties, which ultimately led to the identification of PPAT inhibitors with cellular activity against wild-type E. coli.

Journal of Medicinal Chemistry published new progress about Antibacterial agents. 21901-29-1 belongs to class pyridine-derivatives, and the molecular formula is C6H7N3O2, Category: pyridine-derivatives.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Sepiol, Jadwiga; Tomasik, Piotr published the artcile< Syntheses with aromatic nitramines. VI. Substituent effect in the photolytic rearrangement of nitraminopyridines>, Application In Synthesis of 21901-29-1, the main research area is photochem rearrangement nitraminopyridine; aminonitropyridine; photolytic rearrangement nitraminopyridine; regiochem photochem rearrangement nitraminopyridine; substituent effect photochem rearrangement nitraminopyridine.

Isomeric 2-nitraminopyridines I (R = 3-Me, 4-Me, 5-Me, 6-Me, 3-NO2, 5-NO2, 5-Cl, 3-CO2H) as well as 3,5-dibromo-2-nitraminopyridine (II, R1 = NO2) rearranged on irradiation with a low pressure Hg lamp (253.7 nm) in MeOH. Preference was generally noted for the migration of the side-chain NO2 group to the vicinal β-position. II (R1 = NO2) gave both II (R1 = H) and the pyridone III. The ratio of the preparative and quantum yields of the two products were 2.5 and 3.0, resp.

Acta Chimica Hungarica published new progress about Photorearrangement. 21901-29-1 belongs to class pyridine-derivatives, and the molecular formula is C6H7N3O2, Application In Synthesis of 21901-29-1.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Li, Guo-Xing; Hu, Xiafei; He, Gang; Chen, Gong published the artcile< Photoredox-mediated remote C(sp3)-H heteroarylation of free alcohols>, Application of C7H7NO2, the main research area is alc heteroaryl preparation regioselective chemoselective; heteroarene aliphatic alc heteroarylation.

An efficient and economical method for remote δ C(sp3)-H heteroarylation of free aliphatic alcs., e.g., cyclobutaneethanol using a hypervalent iodine PFBI-OH oxidant under photoredox catalysis has been reported. The reaction sequence involves in situ alcoholysis of PFBI-OH with alc., generation of an alkoxy radical intermediate by SET reduction, 1,5-HAT, and Minisci-type C-C bond formation. This method uses a slight excess of alcs., can facilitate reaction at δ Me and methylene positions, and has been successfully applied to modification of complex drug mols.

Chemical Science published new progress about Alcohols Role: RCT (Reactant), SPN (Synthetic Preparation), RACT (Reactant or Reagent), PREP (Preparation). 93-60-7 belongs to class pyridine-derivatives, and the molecular formula is C7H7NO2, Application of C7H7NO2.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem