Day: October 21, 2022

Wu, Tong; Zhu, Jian; Strickland, Amy; Ko, Kwang Woo; Sasaki, Yo; Dingwall, Caitlin B.; Yamada, Yurie; Figley, Matthew D.; Mao, Xianrong; Neiner, Alicia; Bloom, A. Joseph; DiAntonio, Aaron; Milbrandt, Jeffrey published the artcile< Neurotoxins subvert the allosteric activation mechanism of SARM1 to induce neuronal loss>, Application In Synthesis of 350-03-8, the main research area is neurotoxin allosteric activation mechanism SARM neuronal loss; NAMPT; NMNAT; Vacor; base exchange reaction; mass spectrometry; metabolism; myelin; neurolytic block; sciatic nerve; tibial nerve.

SARM1 is an inducible TIR-domain NAD+ hydrolase that mediates pathol. axon degeneration. SARM1 is activated by an increased ratio of NMN to NAD+, which competes for binding to an allosteric activating site. When NMN binds, the TIR domain is released from autoinhibition, activating its NAD+ hydrolase activity. The discovery of this allosteric activating site led us to hypothesize that other NAD+-related metabolites might activate SARM1. Here, we show the nicotinamide analog 3-acetylpyridine (3-AP), first identified as a neurotoxin in the 1940s, is converted to 3-APMN, which activates SARM1 and induces SARM1-dependent NAD+ depletion, axon degeneration, and neuronal death. In mice, systemic treatment with 3-AP causes rapid SARM1-dependent death, while local application to the peripheral nerve induces SARM1-dependent axon degeneration. We identify 2-aminopyridine as another SARM1-dependent neurotoxin. These findings identify SARM1 as a candidate mediator of environmental neurotoxicity and suggest that SARM1 agonists could be developed into selective agents for neurolytic therapy.

Cell Reports published new progress about Allosterism. 350-03-8 belongs to class pyridine-derivatives, and the molecular formula is C7H7NO, Application In Synthesis of 350-03-8.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Puszko, Aniela published the artcile< UV spectra of 2-halo-4-aminopicolines>, Application In Synthesis of 79055-59-7, the main research area is UV spectra halo derivative aminopyridine.

The UV spectra of 2-halogen-4-aminopicolines were measured in various solvents and the influence of substituent and solvent on position band and intensity are discussed in details.

Prace Naukowe Akademii Ekonomicznej imienia Oskara Langego we Wroclawiu published new progress about Solvent effect. 79055-59-7 belongs to class pyridine-derivatives, and the molecular formula is C6H7BrN2, Application In Synthesis of 79055-59-7.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Zhang, Chun; Santiago, Celine B.; Kou, Lei; Sigman, Matthew S. published the artcile< Alkenyl Carbonyl Derivatives in Enantioselective Redox Relay Heck Reactions: Accessing α,β-Unsaturated Systems>, Formula: C13H15F3N2O, the main research area is arylboronic acid unsaturated carbonyl enantioselective regioselective arylation Heck; aryl unsaturated carbonyl stereoselective preparation.

A highly enantioselective and site-selective Pd-catalyzed arylation of alkenes linked to carbonyl derivatives to yield α,β-unsaturated systems is reported. The high site selectivity is attributed to both a solvent effect and the polarized nature of the carbonyl group, both of which have been analyzed through multidimensional anal. tools. The reaction can be performed in an iterative fashion allowing for a diastereoselective installation of two aryl groups along an alkyl chain.

Journal of the American Chemical Society published new progress about Arylation, stereoselective (regioselective). 1416819-91-4 belongs to class pyridine-derivatives, and the molecular formula is C13H15F3N2O, Formula: C13H15F3N2O.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Amthor, Sebastian; Braun, Hanna; Groene, Julius; Nauroozi, Djawed; Jacob, Timo; Rau, Sven published the artcile< Tailored protective groups for surface immobilization of ruthenium dyes>, Application of C10H8N2, the main research area is phosphonatomethyl silylphosphonatomethyl bipyridine ruthenium complex preparation surface immobilization dye.

McKenna reaction conditions are applied to the [Ru(4,4′-(CH2PO3Et2)2)(bpy)](PF6)2 model chromophore in order to obtain [Ru(4,4′-(CH2PO3TMS2)2)(bpy)](Br2-x)(PF6)x (x = 0-2) (2) by replacing the alkyl moieties of the phosphonates with TMS groups (TMS = trimethylsilyl). The model complex is immobilized onto both NiO powder and NiO electrodes on FTO (fluorine doped tin oxide) using organic solvents. The stability of surface binding in aqueous media and the DSC performance of 2 are tested and compared to those of a conventional dye of structure [Ru(4,4′-(CH2PO3TBA2)2)(bpy)](PF6)2 (1) (TBA = tetra-Bu ammonium). This is the first example of a ruthenium based chromophore with a phosphonic acid silyl-ester being directly immobilized onto a NiO surface. In addition, complex 2 exhibits superior stability towards desorption in aqueous media and at the same time showing improved DSC performance and stability in acetonitrile and a slightly higher dye loading on the electrode surface compared to 1.

Dalton Transactions published new progress about Chromophores. 366-18-7 belongs to class pyridine-derivatives, and the molecular formula is C10H8N2, Application of C10H8N2.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Holladay, Mark W.; Bai, Hao; Li, Yihong; Lin, Nan-Horng; Daanen, Jerome F.; Ryther, Keith B.; Wasicak, James T.; Kincaid, John F.; He, Yun; Hettinger, Anne-Marie; Huang, Peggy; Anderson, David J.; Bannon, Anthony W.; Buckley, Michael J.; Campbell, Jeffrey E.; Donnelly-Roberts, Diana L.; Gunther, Karen L.; Kim, David J. B.; Kuntzweiler, Theresa A.; Sullivan, James P.; Decker, Michael W.; Arneric, Stephen P. published the artcile< Structure-activity studies related to ABT-594, a potent nonopioid analgesic agent: effect of pyridine and azetidine ring substitutions on nicotinic acetylcholine receptor binding affinity and analgesic activity in mice>, Application of C5H4ClNO, the main research area is ABT594 analog nonopioid analgesic structure; nicotinic receptor binding ABT594 analog structure.

Analogs of A-98593 (I) and its enantiomer ABT-594 (II) with diverse substituents on the pyridine ring were prepared and tested for affinity to nicotinic acetylcholine receptor binding sites in rat brain and for analgesic activity in the mouse hot plate assay. Numerous types of modifications were consistent with high affinity for [3H]cytisine binding sites. By contrast, only selected modifications resulted in retention of analgesic potency in the same range as I and II. Analogs of II with one or two Me substituents at the 3-position of the azetidine ring also were prepared and substantially less active in both assays.

Bioorganic & Medicinal Chemistry Letters published new progress about Analgesics. 96630-88-5 belongs to class pyridine-derivatives, and the molecular formula is C5H4ClNO, Application of C5H4ClNO.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Ye, Lina; Fang, Yuanyuan; Ou, Zhongping; Wang, Liping; Xue, Songlin; Lu, Yang; Kadish, Karl M. published the artcile< Axial coordination reactions with nitrogenous bases and determination of equilibrium constants for zinc tetraarylporphyrins containing four β,β′-fused butano and benzo groups in nonaqueous media>, Product Details of C7H7NO, the main research area is zinc tetraarylporphyrin nitrogenous base equilibrium constant.

The axial coordination properties of six zinc tetraarylporphyrins with seven different nitrogenous bases were examined in CH2Cl2 for derivatives containing four β,β′-fused butano or benzo groups and the equilibrium constants (logK) determined using spectral titration methods. The examined compounds are represented as butano(YPh)4PorZn and benzo(YPh)4PorZn, where Por is the porphyrin dianion and Y is a CH3, H or Cl substituent on the para-position of each meso-Ph ring of the macrocycle. The initial four-coordinate butano- and benzoporphyrins will axially bind one nitrogenous base to form five-coordinate derivatives in CH2Cl2 and this leads to a 4-22 nm red-shift of the Soret and Q bands. The logK values range from 1.98 to 4.69 for butano(YPh)4PorZn and from 3.42 to 5.36 for benzo(YPh)4PorZn, with the exact value depending upon the meso and β-substituents of the porphyrin and the conjugate acid dissociation constants (pKa) of the nitrogenous base.

Journal of Porphyrins and Phthalocyanines published new progress about Concentration (process). 350-03-8 belongs to class pyridine-derivatives, and the molecular formula is C7H7NO, Product Details of C7H7NO.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Liu, Juan; Yu, Yuhua; Zhao, Jie; Zhao, Peng; Wen, Xuejun; Zhuang, Zhigang; Lin, Chao published the artcile< Integrating disulfides into a polyethylenimine gene carrier selectively boosts significant transfection activity in lung tissue enabling robust IL-12 gene therapy against metastatic lung cancers>, HPLC of Formula: 2127-03-9, the main research area is integrating disulfide polyethylenimine interleukin human metastatic lung cancer; Disulfide; Interleukin-12; Metastatic lung cancer; Polyethylenimine; Transfection.

Bioreducible polyethylenimines (SSPEIs) are promising non-viral carriers for cancer gene therapy. However, the availability of significant gene transfection activity by SSPEIs remains a challenge. Herein, an essential step was taken to ascertain whether or not the disulfide bonds of SSPEIs play a critical role in promoting significant gene transfection activity in different tissues. Initially, a disulfide-linked linear polyethylenimine (denoted as SSLPEI) consisting of one 5.0 kDa LPEI main chain and three disulfide-linked 5.7 kDa LPEI grafts was designed and prepared to possess similar mol. weight with commercialized 25 kDa LPEI as a pos. control. The SSLPEI could induce superior in vitro transfection activity in different cells to the LPEI control as well as low cytotoxicity. Notably, such enhanced in vitro transfection effect by the SSLPEI was more marked in type-II alveolar epithelial cells compared to different cancer cells. In a Balb/c nude mouse model bearing SKOV-3 tumor, the SSLPEI caused parallel level of transgene expression with the LPEI control in the tumor but significantly higher level in the mouse lung. Furthermore, the SSLPEI and LPEI groups afforded an identical antitumor efficacy against the SKOV-3 tumor via i.v. delivery of a shRNA for silencing VEGF expression in the tumor. However, via i.v. delivery of an interleukin-12 (IL-12) gene into metastatic lung cancers in a C57BL/6 mouse model, the SSLPEI group exerted markedly higher IL-12 expression level in the mouse lung and peripheral blood as compared to the LPEI group, thereby boosting IL-12 immunotherapy against the lung metastasis with longer medium survival time. The results of this work elicit that the disulfide bonds of SSPEIs play a pivotal role in enhancing gene transfection activity selectively in the lung tissue rather than solid tumor, enabling high translational potential of SSPEIs for non-viral gene therapy against metastatic lung cancers.

Materials Science & Engineering, C: Materials for Biological Applications published new progress about Alveolar epithelium. 2127-03-9 belongs to class pyridine-derivatives, and the molecular formula is C10H8N2S2, HPLC of Formula: 2127-03-9.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Harenberg, Johannes H.; Weidmann, Niels; Knochel, Paul published the artcile< Preparation of Functionalized Aryl, Heteroaryl, and Benzylic Potassium Organometallics Using Potassium Diisopropylamide in Continuous Flow>, SDS of cas: 2127-03-9, the main research area is metalation continuous flow generation organopotassium aromatic hetaryl nucleophile; electrophile addition coupling organopotassium aromatic heterocyclic compound; alc ketone thioether silane preparation organopotassium nucleophile addition coupling; arenes; flow chemistry; heteroarenes; lateral metalation; potassium.

Heterocyclic and aromatic compounds were metalated by lithium-free potassium diisopropylamide serving as nucleophiles in carbonyl group addition and coupling reactions, providing access to versatile substituted benzothiazoles, benzothiophenes, benzofurans and functionalized aromatic compounds We report the preparation of lithium-salt-free KDA (potassium diisopropylamide; 0.6 M in hexane) complexed with TMEDA (N,N,N’,N’-tetramethylethylenediamine) and its use for the flow-metalation of (hetero)arenes between -78° and 25° with reaction times between 0.2 s and 24 s and a combined flow rate of 10 mL min-1 using a com. flow setup. The resulting potassium organometallics react instantaneously with various electrophiles, such as ketones, aldehydes, alkyl and allylic halides, disulfides, Weinreb amides, and Me3SiCl, affording functionalized (hetero)arenes in high yields. This flow procedure is successfully extended to the lateral metalation of methyl-substituted arenes and heteroaromatics, resulting in the formation of various benzylic potassium organometallics. A metalation scale-up was possible without further optimization.

Angewandte Chemie, International Edition published new progress about Alcohols Role: SPN (Synthetic Preparation), PREP (Preparation). 2127-03-9 belongs to class pyridine-derivatives, and the molecular formula is C10H8N2S2, SDS of cas: 2127-03-9.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Dong, Yuman; Liu, Peng published the artcile< Reduction-triggered di-block copolymer prodrug for high-performance long-acting tumor-selective killing>, Related Products of 2127-03-9, the main research area is acrylic polyoxyalkylene diblock progrug antitumor agent; Long-acting prodrug; Reduction-triggered drug delivery; Solubility-controlled release; Tumor-selective killing; Tumor-specific.

Long-acting drug delivery systems (DDSs) have attracted interests for tumor chemotherapy. Here, novel reduction-triggered polymer prodrug was designed by conjugation of a high-performance thiolated doxorubicin (DOX-SH) onto the diblock copolymer PEG43-PPDSM43 via the bioreducible cleavable disulfide bond. The resultant polymer prodrug PEG43-PPDSM43-DOX with a DOX content of 33% could be easily self-assembled into nanoparticles of 146 nm. They showed a slow solubility-controlled sustained drug release with a cumulative release of 30.13% within 84 h in the simulated tumor intracellular microenvironment but an ultra-low premature drug leakage of 4.01% in the simulated normal physiol. media. Such slow sustained release is expected to prolong the action time of the active drug. The MTT assays demonstrated the tumor-selective killing performance of the proposed prodrug nanoparticles with an enhanced antitumor efficacy on the tumor HepG2 cells than the free DOX, but no obvious cytotoxicity on the normal L20 cells at the lower dosages.

Colloids and Surfaces, B: Biointerfaces published new progress about Antitumor agents. 2127-03-9 belongs to class pyridine-derivatives, and the molecular formula is C10H8N2S2, Related Products of 2127-03-9.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Weglinski, Zbigniew; Talik, Tadeusz published the artcile< Carboxylation of 2-hydroxypicolines>, Safety of 6-Amino-3-nitro-2-picoline, the main research area is carboxylation hydroxypicoline; pyridinol methyl carboxylation; picoline hydroxy carboxylation; pyridinecarboxylic acid hydroxymethyl.

Treatment of a mixture of 2-hydroxy-3-methylpyridine (I) and anhydrous K2CO3 with 55 atm CO2 at 220° for 9 h gave 87% 2-hydroxy-3-methyl-5-pyridinecarboxylic acid (II). Carboxylation of the Na and K salts of I gave 49.5 and 53% II, resp. Similarly, 2-hydroxy-5-methyl-, 2-hydroxy-6-methyl-, and 2-hydroxy-4-methylpyridine gave 2-hydroxy-5-methyl-3-pyridinecarboxylic acid, 2-hydroxy-6-methyl-3-pyridinecarboxylic acid, and 2-hydroxy-4-methyl-5-pyridinecarboxylic acid, resp. The isomeric hydroxymethylpyridinecarboxylic acids were also prepared by hydrolysis of the corresponding isomeric chlorocyanopicolines. The latter were obtained from isomeric aminopicolines by successive nitration, hydroxylation, chlorination, reduction, and Sandmeyer cyanation.

Roczniki Chemii published new progress about Carboxylation. 22280-62-2 belongs to class pyridine-derivatives, and the molecular formula is C6H7N3O2, Safety of 6-Amino-3-nitro-2-picoline.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem