Category: pyridine-derivatives

Xie, Dongsheng; Lu, Jun; Xie, Jin; Cui, Junjun; Li, Teng-Fei; Wang, Yan-Chao; Chen, Yuan; Gong, Nian; Li, Xin-Yan; Fu, Lei; Wang, Yong-Xiang published the artcile< Discovery and analgesic evaluation of 8-chloro-1,4-dihydropyrido[2,3-b]pyrazine-2,3-dione as a novel potent D-amino acid oxidase inhibitor>, Recommanded Product: 5-Fluoropyridine-2,3-diamine, the main research area is chlorodihydro pyridopyrazine dione preparation amino acid oxidase inhibitor; 5-Azaquinoxaline-2,3-diones; 8-Chloro-1,4-dihydropyrido[2,3-b]pyrazine-2,3-dione; Analgesic effects; D-amino acid oxidase; DAAO inhibitors.

A series of 5-azaquinoxaline-2,3-dione derivatives were synthesized and evaluated on D-amino acid oxidase (DAAO) inhibition as potential α-hydroxylactam-based inhibitors. The potent inhibitory activities in vitro suggested that 5-nitrogen could significantly enhance the binding affinity by strengthening relevant hydrogen bond interactions. The analgesic effects of intrathecal and systemic injection of 8-chloro-1,4-dihydropyrido[2,3-b]pyrazine-2,3-dione, a representative mol. of 5-azaquinoxaline-2,3-dione, were investigated in rodents. This research not only confirmed the analgesic effect of the DAAO inhibitors but provided a new class of chem. entities with oral application potential for the treatment of chronic pain and morphine analgesic tolerance.

European Journal of Medicinal Chemistry published new progress about Analgesics. 212268-13-8 belongs to class pyridine-derivatives, and the molecular formula is C5H6FN3, Recommanded Product: 5-Fluoropyridine-2,3-diamine.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Zhu, Huajian; Li, Wenlong; Shuai, Wen; Liu, Yang; Yang, Limei; Tan, Yuchen; Zheng, Tiandong; Yao, Hong; Xu, Jinyi; Zhu, Zheying; Yang, Dong-Hua; Chen, Zhe-Sheng; Xu, Shengtao published the artcile< Discovery of novel N-benzylbenzamide derivatives as tubulin polymerization inhibitors with potent antitumor activities>, Formula: C6H8N2, the main research area is colchicine binding antitumor safety profile; benzylbenzamide preparation cytotoxicity antitumor mol docking tubulin inhibitor; Anti-vascular; Antitumor; Druggability; N-benzylbenzamide; Tubulin inhibitors.

A series of novel N-benzylbenzamide derivatives I (R = dimethylaminyl, piperidin-1-yl, morpholin-4-yl, etc.; R1 = H, Cl, NO2, (pyridin-4-ylmethyl)aminyl, etc.; R2 = H, NO2; R3 = (3-hydroxy-4-methoxyphenyl)methyl, (3-fluoro-4-methoxyphenyl)methyl, pyridin-4-ylmethyl, etc.; R4 = H, Me), II (X = Y = N, CH) and III were designed and synthesized as tubulin polymerization inhibitors. Among fifty-one target compounds, I, II and III compound I [R = morpholin-4-yl; R1 = F; R2 = H; R3 = (3-hydroxy-4-methoxyphenyl)methyl; R4 = H] (IV) exhibited significant antiproliferative activities with IC50 values ranging from 12 to 27 nM against several cancer cell lines, and possessed good plasma stability and satisfactory physicochem. properties. Mechanism studies demonstrated that IV bound to the colchicine binding site and displayed potent anti-vascular activity. Notably, the corresponding disodium phosphate III exhibited an excellent safety profile with the LD50 value of 599.7 mg/kg (i.v. injection), meanwhile, it significantly inhibited tumor growth and decreased microvessel d. in liver cancer cell H22 allograft mouse model without obvious toxicity. Collectively, IV and III are novel promising anti-tubulin agents with more druggable properties and deserve to be further investigated for cancer therapy.

European Journal of Medicinal Chemistry published new progress about Amines Role: RCT (Reactant), RACT (Reactant or Reagent). 3731-53-1 belongs to class pyridine-derivatives, and the molecular formula is C6H8N2, Formula: C6H8N2.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Sinwat, Nuananong; Witoonsatian, Kriangkrai; Chumsing, Suksan; Suwanwong, Monticha; Kankuntod, Somyod; Jirawattanapong, Pichai; Songserm, Thaweesak published the artcile< Antimicrobial Resistance Phenotypes and Genotypes of Salmonella spp. Isolated from Commercial Duck Meat Production in Thailand and Their Minimal Inhibitory Concentration of Disinfectants>, Recommanded Product: 1-Hexadecylpyridin-1-ium chloride, the main research area is Salmonella disinfectant antimicrobial resistance phenotype genotype duck meat; Salmonella enterica; antimicrobial resistance; disinfectant resistance; meat-type ducks.

Salmonella is an important foodborne bacterium that has become increasingly resistant to critical antimicrobial and disinfectant agents. The aim of this study was to characterize antimicrobial and disinfectant resistance of Salmonella spp. isolated from ducks raised for meat in Nakhon Pathom province, Thailand. A total of 694 fecal samples from ducks were collected in 2018. Of which, 85 samples were pos. for Salmonella (12.2%), and 12 Salmonella serovars were identified from 125 Salmonella isolates. The Altona serovar was the predominant serotype found in this study (36.5%). All isolates showed resistance to at least one class of antimicrobial, and 23.2% displayed multidrug resistance (MDR) phenotype. The blaTEM, aadA2, strA, and dfrA12 genes were detected in antibiotic-resistant strains of Salmonella, whereas the genes within a plasmid-borne qnr family that presented in fluoroquinolone-susceptible Salmonella strains were qnrB (3.8%) and qnrS (1.5%). The min. inhibitory concentrations of benzalkonium chloride (BKC), cetylpyridium chloride (CPC), and hexadecyltrimethyl ammonium bromide (CTAB) ranged between 128 and 512μgg/mL, while that of didecyldimethylammonium chloride (DDAC) was between 32 and 128μg/mL. The presences of qacEΔ1, mdfA, sugE(c), sugE(p), and ydgE genes were less prevalent (0.8-1.6%). Taken together, our results indicate that duck is an important source of Salmonella with antimicrobial resistance in food-producing animals. Active surveillance programs for antimicrobial and disinfectant resistance in duck production are needed for an early detection of resistance strains of public health importance.

Microbial Drug Resistance (New Rochelle, NY, United States) published new progress about Antimicrobial agent resistance. 123-03-5 belongs to class pyridine-derivatives, and the molecular formula is C21H38ClN, Recommanded Product: 1-Hexadecylpyridin-1-ium chloride.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Beller, Matthias; Magerlein, Wolfgang; Indolese, Adriano F.; Fischer, Christine published the artcile< Efficient palladium-catalyzed alkoxycarbonylation of N-heteroaryl chlorides - A practical synthesis of building blocks for pharmaceuticals and herbicides. [Erratum to document cited in CA135:210917]>, Product Details of C6H6ClNO, the main research area is erratum butyl pyridinecarboxylate preparation; butyl pyridinecarboxylate preparation erratum; heteroaryl chloride alkoxycarbonylation palladium phosphine ligand catalyst erratum; alkoxycarbonylation chloropyridine palladium catalyst erratum.

The correct structures are given for Table 5, entry 3, product; Table 7, entry 1, product; Table 7, entry 2, product; and Table 7, entry 3, product.

Synthesis published new progress about Alkoxycarbonylation. 13472-84-9 belongs to class pyridine-derivatives, and the molecular formula is C6H6ClNO, Product Details of C6H6ClNO.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Zhu, Guohua; Huang, Yang; Wang, Chun; Lu, Linxia; Sun, Tongming; Wang, Miao; Tang, Yanfeng; Shan, Doudou; Wen, Shuijin; Zhu, Jinli published the artcile< A novel coumarin-based fluorescence chemosensor for Al3+ and its application in cell imaging>, Reference of 93-60-7, the main research area is coumarin fluorescence chemosensor aluminum cell imaging; Al(3+); Chemosensor; Coumarin; Live cells.

As an efficient turn-on fluorescent chemosensor for Al3+, a new coumarin derivative (CND) has been designed and synthesized by the condensation of 8-formyl-7-hydroxycoumarin with niacin hydrazide. The spectroscopic studies revealed that the sensor CND exhibited a remarkable fluorescence enhancement towards Al3+ with high selectivity and sensitivity in EtOH-HEPES (95:5, volume/volume, pH = 7.40), which was attributed to the photoinduced electron transfer (PET) and -C:N isomerization mechanism. Fluorescence titration calculations data showed that the detection limit and the association constants of CND for Al3+ are 2.51 × 10-7 M and 9.64 × 104 M-1, resp. The results of experiments, including Job’s plot, 1H NMR titration and ESI-MS, revealed that the stoichiometric binding between CND and Al3+ was 1:1. The studies of the pH dependency of CND for Al3+ detection, and the cell imaging suggested the sensor CND could be promisingly applied for the recognition of Al3+ in biol. cells.

Spectrochimica Acta, Part A: Molecular and Biomolecular Spectroscopy published new progress about Fluorescence. 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

Oates, Conor L.; Widegren, Magnus B.; Clarke, Matthew L. published the artcile< Manganese-catalysed transfer hydrogenation of esters>, Application In Synthesis of 93-60-7, the main research area is primary alc preparation manganese catalyst; ester reduction ethanol hydrogen transfer agent.

Manganese catalyzed ester reduction using ethanol as a hydrogen transfer agent in place of dihydrogen is reported. High yields can be achieved for a range of substrates using 1 mol% of a Mn(I) catalyst, with an alkoxide promoter. The catalyst is derived from a tridentate P,N,N ligand.

Chemical Communications (Cambridge, United Kingdom) published new progress about Aliphatic esters Role: RCT (Reactant), RACT (Reactant or Reagent). 93-60-7 belongs to class pyridine-derivatives, and the molecular formula is C7H7NO2, Application In Synthesis of 93-60-7.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Maji, Ankur; Gupta, Shivangi; Maji, Milan; Kundu, Sabuj published the artcile< Well-Defined Phosphine-Free Manganese(II)-Complex-Catalyzed Synthesis of Quinolines, Pyrroles, and Pyridines>, Recommanded Product: 1-(Pyridin-3-yl)ethanone, the main research area is quinoline pyrrole pyridine preparation density functional theory; amino alc ketone manganese complex catalyst.

Herein, authors report a simple, phosphine-free, and inexpensive catalytic system based on a manganese(II) complex for synthesizing different important N-heterocycles such as quinolines, pyrroles and pyridines from amino alcs. and ketones. Several control experiments, kinetic studies, and DFT calculations were carried out to support the plausible reaction mechanism. Authors also detected two potential intermediates in the catalytic cycle using ESI-MS anal. Based on these studies, a metal-ligand cooperative mechanism was proposed.

Journal of Organic Chemistry published new progress about Amino alcohols Role: RCT (Reactant), RACT (Reactant or Reagent). 350-03-8 belongs to class pyridine-derivatives, and the molecular formula is C7H7NO, Recommanded Product: 1-(Pyridin-3-yl)ethanone.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Chandrashekhar, Vishwas G.; Baumann, Wolfgang; Beller, Matthias; Jagadeesh, Rajenahally V. published the artcile< Nickel-catalyzed hydrogenative coupling of nitriles and amines for general amine synthesis>, Category: pyridine-derivatives, the main research area is amine preparation; nitrile amine hydrogenative coupling nickel catalyzed.

A homogeneous nickel catalyst for hydrogenative cross coupling of a range of aromatic, heteroaromatic, and aliphatic nitriles with primary and secondary amines or ammonia to give amines was reported. This general hydrogenation protocol was showcased by straightforward and highly selective synthesis of >230 functionalized and structurally diverse amines including pharmaceutically relevant and chiral products, as well as 15N-isotope labeling applications.

Science (Washington, DC, United States) published new progress about Amines Role: RCT (Reactant), SPN (Synthetic Preparation), RACT (Reactant or Reagent), PREP (Preparation). 3731-53-1 belongs to class pyridine-derivatives, and the molecular formula is C6H8N2, Category: pyridine-derivatives.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Robke, Lucas; Rodrigues, Tiago; Schroeder, Peter; Foley, Daniel J.; Bernardes, Goncalo J. L.; Laraia, Luca; Waldmann, Herbert published the artcile< Discovery of 2,4-dimethoxypyridines as novel autophagy inhibitors>, Reference of 832735-54-3, the main research area is dimethoxy pyridine derivative preparation autophagy inhibitor structure.

Autophagy is a catabolic process, which mediates degradation of cellular components and has important roles in health and disease. Therefore, small mol. modulators of autophagy are in great demand. Herein, we describe a phenotypic high-content screen for autophagy inhibitors, which led to the discovery of a dimethoxypyridine-based class of autophagy inhibitors, which derive from previously reported, natural product-inspired MAP4K4 inhibitors. Comprehensive structure-activity relationship studies led to a potent compound, and biol. validation experiments indicated that the mode of action was upstream or independent of mTOR.

Tetrahedron published new progress about Apoptosis. 832735-54-3 belongs to class pyridine-derivatives, and the molecular formula is C18H22BNO3, Reference of 832735-54-3.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem