Tag: M.W=200-250

Koovits, Paul J.; Dessoy, Marco A.; Matheeussen, An; Maes, Louis; Caljon, Guy; Mowbray, Charles E.; Kratz, Jadel M.; Dias, Luiz C. published the artcile< Structure-activity relationship of 4-azaindole-2-piperidine derivatives as agents against Trypanosoma cruzi>, Synthetic Route of 1050501-88-6, the main research area is azaindole piperidine structure activity relationship trypanosoma cruzi chagas disease; Azaindole; Chagas disease; Drug discovery; Neglected diseases.

The structure-activity relationship of a 4-Azaindole-2-piperidine compound selected from GlaxoSmithKline’s recently disclosed open-resource “”Chagas box”” and possessing moderate activity against Trypanosoma cruzi, the parasite responsible for Chagas disease, is presented. Despite considerable medicinal chem. efforts, a suitably potent and metabolically stable compound could not be identified to advance the series into in vivo studies. This research should be of interest to those in the area of neglected diseases and in particular anti-kinetoplastid drug discovery.

Bioorganic & Medicinal Chemistry Letters published new progress about Chagas disease. 1050501-88-6 belongs to class pyridine-derivatives, and the molecular formula is C5H4BrClN2, Synthetic Route of 1050501-88-6.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Schuster, Georg; Lindner, Wolfgang published the artcile< Comparative characterization of hydrophilic interaction liquid chromatography columns by linear solvation energy relationships>, Related Products of 21876-43-7, the main research area is hydrophilic interaction liquid chromatog column linear solvation energy relationship; acid organic hydrophilic interaction LC linear solvation energy relation; base organic hydrophilic interaction LC linear solvation energy relation.

Twenty-two com. available and home-made stationary phases with different surface modifications were compared under hydrophilic interaction liquid chromatog. (HILIC) conditions. The column set comprised neutral, basic, acidic, zwitterionic and mixed surface modifications. Retention data of 68 differently structured test solutes were acquired to generate retention models based on a linear solvation energy relation (LSER) approach. A recently modified solvation parameter model with two addnl. mol. descriptors was evaluated in terms of its universal applicability when electrostatic forces are enabled in addition to predominant partition phenomena. The suggested method could not be confirmed to be a standardized way to characterize HILIC systems when different operating conditions are applied. However, the significant contribution of the recently introduced charge descriptors (D- and D+) on explaining the interactions within HILIC systems was confirmed. The solvation parameter model is a useful tool in column development, to affirm or dismiss the preceding educated guess on how certain immobilized ligands will behave. Acidic modified surfaces (stationary phases) exhibit a very small hydrogen bond acceptor property and are less versatile when it comes to an even distribution of solutes along the retention window. Also, basic and neutral columns are more preferable for HILIC applications and might explain why only a limited variety of strong acidic modified HILIC columns, although found in literature, are available com.

Journal of Chromatography A published new progress about Electrostatic force. 21876-43-7 belongs to class pyridine-derivatives, and the molecular formula is C9H13NO3S, Related Products of 21876-43-7.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Conejos-Sanchez, I.; Gallon, E.; Nino-Pariente, A.; Smith, J. A.; De la Fuente, A. G.; Di Canio, L.; Pluchino, S.; Franklin, R. J. M.; Vicent, M. J. published the artcile< Polyornithine-based polyplexes to boost effective gene silencing in CNS disorders>, Related Products of 2127-03-9, the main research area is polyornithine siRNA polyplex central nervous system disorder.

Gene silencing therapies have successfully suppressed the translation of target proteins, a strategy that holds great promise for the treatment of central nervous system (CNS) disorders. Advances in the current knowledge on multimol. delivery vehicles are concentrated on overcoming the difficulties in delivery of small interfering (si)RNA to target tissues, which include anatomical accessibility, slow diffusion, safety concerns, and the requirement for specific cell uptake within the unique environment of the CNS. The present work addressed these challenges through the implementation of polyornithine derivatives in the construction of polyplexes used as non-viral siRNA delivery vectors. Physicochem. and biol. characterization revealed biodegradability and biocompatibility of our polyornithine-based system and the ability to silence gene expression in primary oligodendrocyte progenitor cells (OPCs) effectively. In summary, the well-defined properties and neurol. compatibility of this polypeptide-based platform highlight its potential utility in the treatment of CNS disorders.

Nanoscale published new progress about Biocompatibility. 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

Serrano-Ruiz, Juan Carlos; Campelo, Juan M.; Francavilla, Matteo; Romero, Antonio A.; Luque, Rafael; Menendez-Vazquez, Carmen; Garcia, Ana B.; Garcia-Suarez, Eduardo J. published the artcile< Efficient microwave-assisted production of furfural from C5 sugars in aqueous media catalyzed by Broensted acidic ionic liquids>, SDS of cas: 21876-43-7, the main research area is ionic liquid xylose hydrolysis dehydration catalyst furfural microwave.

Small amounts of SO3H-functionalized room temperature synthesized ionic liquids efficiently dehydrate aqueous xylose to furfural under microwave heating at mild reaction conditions. The RT-ionic liquid catalysts were also found to be effective catalysts for the two step one-pot simultaneous hydrolysis and dehydration of a lignocellulosic waste biorefinery-derived syrup enriched in C5 sugar oligomers.

Catalysis Science & Technology published new progress about Bronsted acidity. 21876-43-7 belongs to class pyridine-derivatives, and the molecular formula is C9H13NO3S, SDS of cas: 21876-43-7.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Sanders, Georgine M.; Van Dijk, M.; Van der Plas, H. C. published the artcile< Reactions of haloquinolizinium bromides with diethylamine>, Recommanded Product: Methyl 3-bromo-2-pyridinecarboxylate, the main research area is quinolizinium bromide diethylamine reaction.

The reactions of quinolizinium bromide (QB) and its four monobromo derivatives with diethylamine have been investigated. For Br in position 2 or 4, substitution is the main process, whereas for Br in positions 1 and 3 quant. ring opening is found. The substituted pyridylbutadienes formed by ring opening, are cis-trans-butadienes, which isomerize into the all-trans forms. The steric course of the ring opening is explained.

Journal of Heterocyclic Chemistry published new progress about 53636-56-9. 53636-56-9 belongs to class pyridine-derivatives, and the molecular formula is C7H6BrNO2, Recommanded Product: Methyl 3-bromo-2-pyridinecarboxylate.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Kuwata, Yoshiyuki; Sonoda, Motohiro; Tanimori, Shinji published the artcile< Facile Synthesis of Phenanthridinone Alkaloids via Suzuki-Miyaura Cross-coupling>, Electric Literature of 53636-56-9, the main research area is phenanthridinone alkaloid crinasiadine dihydrobicolorine trisphaeridine bicolorine facile synthesis; aminophenylboronic acid Suzuki Miyaura cross coupling bromobenzoate bromoheteroarenecarboxylate.

Phenanthridinone alkaloids crinasiadine (I) and N-alkylcrinasiadines II [R = CH2CH2CHMe2, CH2CH2CO2Et, CH2CH2Ph, CH2CH2CH2CO2Et] have been synthesized based on palladium-catalyzed tandem C-C and C-N bond formation starting from 2-aminophenylboronic acid and 2-bromobenzoate in short steps. Related alkaloids, 5,6-dihydrobicolorine (III), trisphaeridine (IV), and bicolorine (V) have also been synthesized.

Journal of Heterocyclic Chemistry published new progress about Alkaloids Role: RCT (Reactant), SPN (Synthetic Preparation), RACT (Reactant or Reagent), PREP (Preparation) (phenanthridine). 53636-56-9 belongs to class pyridine-derivatives, and the molecular formula is C7H6BrNO2, Electric Literature of 53636-56-9.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Tatikonda, Rajendhraprasad; Cametti, Massimo; Kalenius, Elina; Famulari, Antonino; Rissanen, Kari; Haukka, Matti published the artcile< Mononuclear Ru(II) PolyPyridyl Water Oxidation Catalysts Decorated with Perfluoroalkyl C8H17-Tag Bearing Chains>, Application In Synthesis of 1762-41-0, the main research area is mononuclear ruthenium polypyridyl complex preparation crystal mol structure; water oxidation catalyst decorated perfluoroalkyl polypyridyl mononuclear ruthenium complex; perfluoroundecyl polypyridyl ruthenium complex preparation crystal mol structure.

A set of novel polypyridyl Ru(II) complexes 1-7, decorated with one, two or three C8F17 tags have been synthesized and characterized by NMR, UV/Vis spectroscopy and, in the case of series of complexes 1-3, 5 and 7 by x-ray diffraction on single crystals. Solid state structures of 3, 5 and 7 were also subjected to computational DFT study in order to gain insights into the effect of a different number of perfluorinated tags on their stability in the solid-state. The complexes are stable in solution under strongly oxidative conditions, do keep catalytic activity in their aquo forms (1′-7′) comparing well with parent complex 8′, and their amphiphilic nature could allow for their incorporation in fluorous media and interfaces.

European Journal of Inorganic Chemistry published new progress about Crystal structure. 1762-41-0 belongs to class pyridine-derivatives, and the molecular formula is C10H6Cl2N2, Application In Synthesis of 1762-41-0.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Huang, Zhi; Zhou, Wei; Li, Yongtao; Cao, Mei; Wang, Tianqi; Ma, Yakun; Guo, Qingxiang; Wang, Xin; Zhang, Chao; Zhang, Chenglan; Shen, Wenzhi; Liu, Yanhua; Chen, Yanan; Zheng, Jianyu; Yang, Shengyong; Fan, Yan; Xiang, Rong published the artcile< Novel hybrid molecule overcomes the limited response of solid tumours to HDAC inhibitors via suppressing JAK1-STAT3-BCL2 signalling>, Reference of 220731-04-4, the main research area is breast ovarian cancer HDAC inhibitor JAK1 STAT3 BCL2 signaling; CDK4/6; HDAC1; JAK1; inhibitor; solid tumour.

Despite initial progress in preclin. models, most known histone deacetylase inhibitors (HDACis) used as a single agent have failed to show clin. benefits in nearly all types of solid tumors. Hence, the efficacy of HDACis in solid tumors remains uncertain. Herein, we developed a hybrid HDAC inhibitor that sensitized solid tumors to HDAC-targeted treatment. Methods: A hybrid mol., Roxyl-zhc-84 was designed and synthesized with novel architecture. The pharmacokinetics and toxicity of Roxyl-zhc-84 were analyzed. Results: Roxyl-zhc-84 showed excellent pharmacokinetics and low toxicity. The novel hybrid inhibitor Roxyl-zhc-84 induced cell apoptosis and G1-phase arrest in breast cancer and ovarian cancer cell lines. In three mouse models, oral administration of Roxyl-zhc-84 led to significant tumor regression without obvious toxicity. Moreover, Roxyl-zhc-84 dramatically improved the limited response of traditional HDAC inhibitors in solid tumors via overcoming JAK1-STAT3-BCL2-mediated drug resistance. Roxyl-zhc-84 treatment exhibited vastly superior efficacy than the combination of HDAC and JAK1 inhibitors both in vitro and in vivo. Conclusion: Concurrent inhibition of HDAC and CDK using Roxyl-zhc-84 with addnl. JAK1 targeting resolved the limited response of traditional HDAC inhibitors in solid tumors via overcoming JAK1-STAT3-BCL2-mediated drug resistance, providing a rational multi-target treatment to sensitize solid tumors to HDACi therapy.

Theranostics published new progress about Acetylated histone H3 Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 220731-04-4 belongs to class pyridine-derivatives, and the molecular formula is C10H15N3O2, Reference of 220731-04-4.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Kooyman, E. C.; Wibaut, J. P. published the artcile< Pyridine and quinoline derivatives. LX. The orientation of the CO2C2H5 group in the condensation product of malonic ester and β-aminocrotonic acid ester>, Product Details of C9H9Cl2NO2, the main research area is .

In the 2-methyl-4,6-dihydroxypyridinecarboxylate described by Knoevenagel and Fries (Ber. 31, 767(1898)), the position of the carboxylate group was unknown. The location of this group at 5 rather than at 3 was established by the following reactions: The original condensation product, heated with POCl3 at 120° in a sealed tube for 4 hrs., yielded a mixture of the acid chloride (I) and the Et ester (II) of 2-methyl-4,6-dichloro-5-pyridinecarboxylic acid, which could be separated by fractional distillation at 1 mm. The first fraction b. 97-104°, and after a 2nd distillation was obtained as a clear, colorless oil which solidified at 14.8°. The analyses agreed fairly well with C7H4ONCl3. On heating with H2O, HCl was split off, and the free acid was obtained. The compound was therefore believed to be I. The 2nd fraction b. 113-16°. It was obtained in 30% yield as white needles, m. 56° (50% EtOH), which were readily soluble in Et2O and EtOH, and sparingly soluble in H2O. It was identified as II. The free acid obtained from the ester by saponification m. 151.5° (dilute HCl) and was slightly soluble in H2O, very slightly soluble in HCl, but readily soluble in Et2O and EtOH. By catalytic reduction of II in absolute EtOH with Pd chloride and KOAc, the Cl was removed, and Et 2-methyl-5-pyridinecarboxylate (III) was obtained in 72% yield as a colorless oil b2 97° (Graf, C.A. 26, 1932). By saponification of III with KOH, preparation of the Cu salt, and decomposition with H2S, the free acid (IV) was obtained. It was purified by sublimation at 180°/35 mm. and m. 209-10°. It was identified by mixed m.p. with a sample prepared from 2-methyl-5-ethylpyridine. The amide (V), m. 196°, was prepared from III by shaking with NH3 according to the method of Graf. The picrate of the ester m. 170-1° (light yellow needles from alc. picric acid). The amide and the picrate showed no m.p. depression when mixed with the corresponding amide and picrate prepared from the ester obtained from 2-methyl-5-ethylpyridine.

Recueil des Travaux Chimiques des Pays-Bas et de la Belgique published new progress about 86129-63-7. 86129-63-7 belongs to class pyridine-derivatives, and the molecular formula is C9H9Cl2NO2, Product Details of C9H9Cl2NO2.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Parvanak Boroujeni, Kaveh; Shojaei, Pegah published the artcile< Poly(4-vinylpyridine)-supported dual acidic ionic liquid: an environmentally friendly heterogeneous catalyst for the one-pot synthesis of 4,4'-(arylmethylene)bis(3-methyl-1-phenyl-1H-pyrazol-5-ols)>, Formula: C9H13NO3S, the main research area is sulfobutylpyridinium sulfate as catalyst Knoevenagel condensation Michael addition.

A poly(4-vinylpyridine)-supported Bronsted ionic liquid was easily prepared from its starting materials and used as a novel, highly efficient, and reusable heterogeneous catalytic system for the synthesis of 4,4′-(arylmethylene)bis(3-methyl-1-phenyl-1H-pyrazol-5-ol derivatives) by a condensation reaction between aromatic aldehydes and 2 equiv of 3-methyl-l-phenyl-5-pyrazolone. The synthesis of the target compound (catalyst) was achieved by a reaction of 1,2-oxathiane 2,2-dioxide (1,4-butanesultone) with 4-Vinylpyridine divinylbenzene copolymer and a subsequent anion exchange. The catalyst thus formed was a polymer-supported 1-(4-sulfobutyl)pyridinium sulfate ionic liquid The reaction products thus formed included 4,4′-(phenylmethylene)bis[3-methyl-1-phenyl-1H-pyrazol-5-ol] derivatives, a furan derivative [4,4′-[(2-furanyl)methylene]bis[3-methyl-1-phenyl-1H-pyrazolo-5-ol]], a thiophene derivative [4,4′-[(2-thienyl)methylene]bis[3-methyl-1-phenyl-1H-pyrazolo-5-ol]].

Turkish Journal of Chemistry published new progress about Addition reaction. 21876-43-7 belongs to class pyridine-derivatives, and the molecular formula is C9H13NO3S, Formula: C9H13NO3S.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem