Month: October 2022

Fang, Lei; Zhao, Zitong; Wang, Jue; Xiao, Ping; Sun, Xiangshi; Ding, Yaping; Zhang, Pengcheng; Wang, Dangge; Li, Yaping published the artcile< Light-controllable charge-reversal nanoparticles with polyinosinic-polycytidylic acid for enhancing immunotherapy of triple negative breast cancer>, SDS of cas: 2127-03-9, the main research area is charge reversal nanoparticle polyinosinic polycytidylic acid delivery cancer immunotherapy; Cancer immunotherapy; Charge-reversal; Nanoparticles; Photodynamic therapy; Polyinosinic-polycytidylic acid; ROS-responsive; Triple negative breast cancer; Tumor microenvironment.

Nucleic acid drugs are highly applicable for cancer immunotherapy with promising therapeutic effects, while targeting delivery of these drugs to disease lesions remains challenging. Cationic polymeric nanoparticles have paved the way for efficient delivery of nucleic acid drugs, and achieved stimuli-responsive disassembly in tumor microenvironment (TME). However, TME is highly heterogeneous between individuals, and most nanocarriers lack active-control over the release of loaded nucleic acid drugs, which will definitely reduce the therapeutic efficacy. Herein, we have developed a light-controllable charge-reversal nanoparticle (LCCN) with controlled release of polyinosinic-polycytidylic acid [Poly(I:C)] to treat triple neg. breast cancer (TNBC) by enhanced photodynamic immunotherapy. The nanoparticles keep suitably pos. charge for stable loading of Poly(I:C), while rapidly reverse to neg. charge after near-IR light irradiation to release Poly(I:C). LCCN-Poly(I:C) nanoparticles trigger effective phototoxicity and immunogenic cell death on 4T1 tumor cells, elevate antitumor immune responses and inhibit the growth of primary and abscopal 4T1 tumors in mice. The approach provides a promising strategy for controlled release of various nucleic acid-based immune modulators, which may enhance the efficacy of photodynamic immunotherapy against TNBC.

Acta Pharmaceutica Sinica B published new progress about Antitumor agents. 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

Fontaine, Fanny; Hequet, Arnaud; Voisin-Chiret, Anne-Sophie; Bouillon, Alexandre; Lesnard, Aurelien; Cresteil, Thierry; Jolivalt, Claude; Rault, Sylvain published the artcile< First identification of boronic species as novel potential inhibitors of the Staphylococcus aureus NorA efflux pump>, Synthetic Route of 832735-54-3, the main research area is boron compound transport protein NorA Staphylococcus.

Overexpression of efflux pumps is an important mechanism of bacterial resistance that results in the extrusion of antimicrobial agents outside the bacterial cell. Inhibition of such pumps appears to be a promising strategy that could restore the potency of existing antibiotics. The NorA efflux pump of Staphylococcus aureus confers resistance to a wide range of unrelated substrates, such as hydrophilic fluoroquinolones, leading to a multidrug-resistance phenotype. Here, 150 heterocyclic boronic species were evaluated for their activity against susceptible and resistant strains of S. aureus. Twenty-four hit compounds, although inactive when tested alone, were found to potentiate ciprofloxacin activity by a 4-fold increase at concentrations ranging from 0.5 to 8 μg/mL against S. aureus 1199B, which overexpresses NorA. Boron-free analogs showed no biol. activity, thus revealing that the boron atom is crucial for biol. activity. This work describes the first reported efflux pump inhibitory activity of boronic acid derivatives

Journal of Medicinal Chemistry published new progress about Antibacterial agents. 832735-54-3 belongs to class pyridine-derivatives, and the molecular formula is C18H22BNO3, Synthetic Route of 832735-54-3.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Hameed P, Shahul; Patil, Vikas; Solapure, Suresh; Sharma, Umender; Madhavapeddi, Prashanti; Raichurkar, Anandkumar; Chinnapattu, Murugan; Manjrekar, Praveena; Shanbhag, Gajanan; Puttur, Jayashree; Shinde, Vikas; Menasinakai, Sreenivasaiah; Rudrapatana, Suresh; Achar, Vijayashree; Awasthy, Disha; Nandishaiah, Radha; Humnabadkar, Vaishali; Ghosh, Anirban; Narayan, Chandan; Ramya, V. K.; Kaur, Parvinder; Sharma, Sreevalli; Werngren, Jim; Hoffner, Sven; Panduga, Vijender; Kumar, C. N. Naveen; Reddy, Jitendar; Kumar KN, Mahesh; Ganguly, Samit; Bharath, Sowmya; Bheemarao, Ugarkar; Mukherjee, Kakoli; Arora, Uma; Gaonkar, Sheshagiri; Coulson, Michelle; Waterson, David; Sambandamurthy, Vasan K.; de Sousa, Sunita M. published the artcile< Novel N-Linked Aminopiperidine-Based Gyrase Inhibitors with Improved hERG and in Vivo Efficacy against Mycobacterium tuberculosis>, Safety of 5-Fluoropyridine-2,3-diamine, the main research area is aminopiperidinyl quinolone naphthyridone Mycobacterium tuberculosis bactericide DNA gyrase inhibitor.

DNA gyrase is a clin. validated target for developing drugs against Mycobacterium tuberculosis (Mtb). Despite the promise of fluoroquinolones (FQs) as anti-tuberculosis drugs, the prevalence of pre-existing resistance to FQs is likely to restrict their clin. value. We describe a novel class of N-linked aminopiperidinyl alkyl quinolones and naphthyridones that kills Mtb by inhibiting the DNA gyrase activity. The mechanism of inhibition of DNA gyrase was distinct from the fluoroquinolones, as shown by their ability to inhibit the growth of fluoroquinolone-resistant Mtb. Biochem. studies demonstrated this class to exert its action via single-strand cleavage rather than double-strand cleavage, as seen with fluoroquinolones. The compounds are highly bactericidal against extracellular as well as intracellular Mtb. Lead optimization resulted in the identification of potent compounds with improved oral bioavailability and reduced cardiac ion channel liability. Compounds from this series are efficacious in various murine models of tuberculosis (e.g., compound I).

Journal of Medicinal Chemistry published new progress about Antibacterial agents. 212268-13-8 belongs to class pyridine-derivatives, and the molecular formula is C5H6FN3, Safety of 5-Fluoropyridine-2,3-diamine.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Buttelmann, Bernd; Alanine, Alexander; Bourson, Anne; Gill, Ramanjit; Heitz, Marie-Paule; Mutel, Vincent; Pinard, Emmanuel; Trube, Gerhard; Wyler, Rene published the artcile< 2-(3,4-Dihydro-1H-isoquinolin-2yl)-pyridines as a novel class of NR1/2B subtype selective NMDA receptor antagonists>, Related Products of 79055-59-7, the main research area is NMDA receptor antagonist structure activity relationship design.

Recently, we disclosed 4-aminoquinolines as structurally novel NR1/2B subtype selective NMDA receptor antagonists. We would now like to report our findings on structurally related pyridine analogs. The SAR developed in this series resulted in the discovery of high affinity antagonists which are selective (vs α1 and M1 receptors) and active in vivo.

Bioorganic & Medicinal Chemistry Letters published new progress about Drug design. 79055-59-7 belongs to class pyridine-derivatives, and the molecular formula is C6H7BrN2, Related Products of 79055-59-7.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Zhang, Rui-Qian; Liu, Zhan-Qing; Luo, Yan-Ling; Xu, Feng; Chen, Ya-Shao published the artcile< Tri-stimuli responsive carbon nanotubes covered by mesoporous silica graft copolymer multifunctional materials for intracellular drug delivery>, Application In Synthesis of 2127-03-9, the main research area is carbon silica graft copolymer multifunctional material intracellular drug delivery.

To overcome premature drug leakage and instability in drug delivery systems, we designed tri-stimuli responsive multiwalled carbon nanotubes covered by mesoporous silica graft poly(N-isopropylacrylamide-block-poly(2-(4-formylbenzoyloxy)) Et methacrylate) multifunctional materials via disulfide linkages (MWCNTs@MSN-s-s-g-PNIPAM-b-PFBEMA). The multifunctional materials could covalently bind and phys. load anticancer drug doxorubicin (DOX), and exhibited pH-, temperature- and reductant-induced multi-stimuli responsiveness, significantly enhancing drug loading capacity and improving the release dynamics of drug. The DOX-loaded multifunctional materials exhibited the optimal release behavior in cancer environments compared with in normal cells upon simultaneously triggered by these stimuli. It meant that the MWCNTs@MSN-s-s-g-PNIPAM-b-PFBEMA could serve as efficient gatekeepers to control the mesopore on-off and thus to modulate drug release. The multifunctional materials were proved to be low toxic, whereas the DOX-loaded counterparts had almost the same toxicity as free DOX to cancer cells. Therefore, the developed multifunctional materials can be used as promising drug controlled delivery platforms for cancer therapy.

Journal of Industrial and Engineering Chemistry (Amsterdam, Netherlands) published new progress about Binding energy. 2127-03-9 belongs to class pyridine-derivatives, and the molecular formula is C10H8N2S2, Application In Synthesis of 2127-03-9.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Nallagonda, Rajender; Musaev, Djamaladdin G.; Karimov, Rashad R. published the artcile< Light-Promoted Dearomative Cross-Coupling of Heteroarenium Salts and Aryl Iodides via Nickel Catalysis>, Computed Properties of 93-60-7, the main research area is dihydropyridine aryl preparation regioselective; aryl iodide pyridinium dearomative cross coupling nickel iridium photocatalyst.

Herein, the coupling of aryl iodides, e.g., Ph iodide with pyridinium and related heteroarenium salts, e.g., I catalyzed by Ni/bpp and an Ir photocatalyst using Zn as a terminal reductant was reported. This methodol. tolerates a wide range of functional groups and allows the coupling of aryl and heteroaryl iodides, thus significantly expanding the scope of nitrogen heterocycle scaffolds, e.g., II that could be prepared through dearomatization of heteroarenes. The reaction products have been further functionalized to prepare various nitrogen heterocycles. Initial mechanistic studies indicate that the reaction described herein goes through a unique mechanism involving dimers of dihydroheteroarenes.

ACS Catalysis published new progress about Aryl iodides 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, Computed Properties of 93-60-7.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Wang, Qing-Dong; Zhang, Si-Xuan; Zhang, Zhuo-Wen; Wang, Ying; Ma, Mengtao; Chu, Xue-Qiang; Shen, Zhi-Liang published the artcile< Palladium-Catalyzed Sonogashira Coupling of a Heterocyclic Phosphonium Salt with a Terminal Alkyne>, Safety of 3-(Methoxycarbonyl)pyridine, the main research area is palladium copper catalyst Sonogashira coupling heterocyclic phosphonium terminal alkyne; pyridine quinoline pyrazine quinoxaline alkynyl preparation functionalized.

An efficient Sonogashira coupling of a heterocyclic phosphonium salt with a terminal alkyne via C-P bond cleavage was developed. The reactions proceeded smoothly in the presence of palladium catalyst, copper(I) iodide, and N,N-diisopropylethylamine (DIPEA) in N-methyl-2-pyrrolidone (NMP) at 100°C for 12 h, producing the corresponding alkynyl-substituted pyridine, quinoline, pyrazine, and quinoxaline in moderate to good yields with wide substrate scope and broad functional group tolerance. In addition, gram-scale synthesis could also be achieved, and the reaction could be applied to the functionalization of alkyne-containing complex mols. derived from sugars and pharmaceutical and naturally occurring products (e.g., estrone, D-galactopyranose, menthol, and ibuprofen).

Organic Letters published new progress about Alkynes, α- Role: RCT (Reactant), RACT (Reactant or Reagent). 93-60-7 belongs to class pyridine-derivatives, and the molecular formula is C7H7NO2, Safety of 3-(Methoxycarbonyl)pyridine.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Doan, Viet Sang; Saingam, Prakit; Yan, Tao; Shin, Sangwoo published the artcile< A Trace Amount of Surfactants Enables Diffusiophoretic Swimming of Bacteria>, Name: 1-Hexadecylpyridin-1-ium chloride, the main research area is surfactant bacteria diffusionphoresis; bacteria; biofilms; diffusiophoresis; surface charge; surfactants.

From birth to health, surfactants play an essential role in the authors’ lives. Due to the importance, their environmental impacts are well understood. One of the aspects that has been extensively studied is their impact on bacteria, particularly on their motility. Here, the authors uncover an alternate chemotactic strategy triggered by surfactants-diffusiophoresis. Even a trace amount of ionic surfactants, down to a single ppm level, can promote the bacterial diffusiophoresis by boosting the surface charge of the cells. Because diffusiophoresis is driven by the surface-solute interactions, surfactant-enhanced diffusiophoresis is observed regardless of the types of bacteria. Whether Gram-pos. or -neg., flagellated or nonflagellated, the surfactants enable fast migration of freely suspended bacteria, suggesting a ubiquitous locomotion mechanism that has been largely overlooked. The authors also demonstrate the implication of surfactant-enhanced bacterial diffusiophoresis on the rapid formation of biofilms in flow networks, suggesting environmental and biomedical implications.

ACS Nano published new progress about Bacteria. 123-03-5 belongs to class pyridine-derivatives, and the molecular formula is C21H38ClN, Name: 1-Hexadecylpyridin-1-ium chloride.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Chutvirasakul, Boonta; Nuchtavorn, Nantana; Macka, Mirek; Suntornsuk, Leena published the artcile< Distance-based paper device using polydiacetylene liposome as a chromogenic substance for rapid and in-field analysis of quaternary ammonium compounds>, Formula: C21H38ClN, the main research area is paper device polydiacetylene liposome chromogenic substance quaternary ammonium compound; Distance-based microfluidic paper-based device; In-field analysis; Polydiacetylene; Quaternary ammonium compounds.

This work presents an affordable distance-based microfluidic paper-based device (μPAD), using polydiacetylene (PDA) liposome as a chromogenic substance with a smartphone-based photo editor, for rapid and in-field anal. of quaternary ammonium compounds (QACs) (e.g., didecyldimethylammonium chloride (DDAC), benzyldimethyltetradecyl ammonium chloride (BAC), and cetylpyridinium chloride (CPC)). In-field anal. of these compounds is important to ensure their antimicrobial activity and user safety since they are widely used as disinfectants in households and hospitals. The μPAD featured a thermometer-like shape consisting of a sample reservoir and a microchannel as the detection zone, which was pre-deposited with PDA liposome. The color change from blue to red appeared in the presence of QACs and the color bar lengths were proportional to the QAC concentrations Reactions of QACs with the PDA required a specific pH range (from pH 4.0 to 10.0) and a readout time of 7 min. Anal. performance characteristics of the device were tested with DDAC, BAC, and CPC showing acceptable specificity, accuracy (96.1-109.4%), and precision (%RSDs ≤ 9.3%). Limits of detection and quantitation were at 20-80 and 70 to 250μM, resp. Feasibility of the newly developed device was demonstrated for in-field anal. of QACs in fumigation solution providing comparable results with those obtained from a colorimetric assay (P > 0.05). The proposed device shows potentials for further applications of other analytes since it offers speed, simplicity, and affordability for in-field anal., especially in remote areas where expertise, resources, and infrastructures are limited.

Analytical and Bioanalytical Chemistry published new progress about Colorimetry. 123-03-5 belongs to class pyridine-derivatives, and the molecular formula is C21H38ClN, Formula: C21H38ClN.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Nagata, Kojiro; Otsuji, Naoko; Akagi, Soichiro; Fujii, Sho; Kitamura, Noboru; Yoshimura, Takashi published the artcile< Synthesis, Structures, and Photoluminescent Properties of Tricyanidonitridorhenium(V) Complexes with Bipyridine-Type Ligands>, Application of C10H6Cl2N2, the main research area is crystal structure rhenium nitrido cyano substituted bipyridine; rhenium tricyanidonitrido bipyridine preparation electrochem redox luminescence charge transfer.

Tricyanidonitridorhenium(V) complexes with 2,2′-bipyridine (bpy) derivatives in which the 4 and 4′ positions were substituted by X, [ReN(CN)3(X2bpy)]- (X = NMe2, NH2, OMe, Me, Cl, and Br), were newly synthesized and characterized. The structures of the new complexes were determined by single-crystal x-ray anal. UV-visible spectra of the complexes in DMSO showed that the peak maximum wavelengths of Re-to-π* bpy-type-ligand charge transfer were at 474-542 nm. Cyclic voltammograms in Bu4NPF6-DMSO showed 1-electron oxidation and reduction waves corresponding to the Re(VI/V) and X2bpy0/- processes, resp. The new complexes and [ReN(CN)3bpy]- showed photoluminescence in the crystalline phase at 295 and 80 K and in DMSO at 295 K. The origin of the emission in DMSO was attributed to the triplet nature of the Re-to-π* bpy-type-ligand charge-transfer transition. D. functional theory calculations showed that the highest occupied and lowest unoccupied MOs were primarily localized on the dxy orbital of the Re and π* orbitals of the bpy-type ligand, resp. Tricyanidonitridorhenium(V) complexes with 2,2′-bipyridine (bpy) derivatives were newly synthesized and characterized. The new complexes and [ReN(CN)3bpy]- showed photoluminescence. The origin of the emission was attributed to the triplet nature of the Re-to-π* bpy-derivative charge-transfer transition.

Inorganic Chemistry published new progress about Charge transfer transition. 1762-41-0 belongs to class pyridine-derivatives, and the molecular formula is C10H6Cl2N2, Application of C10H6Cl2N2.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem