Tag: M.W=200-250

He, Chengzhi; Li, Shuai; Gao, Xiaoqing; Xiao, Adam; Hu, Chunguang; Hu, Xiaodong; Hu, Xiaotang; Li, Hongbin published the artcile< Direct observation of the fast and robust folding of a slipknotted protein by optical tweezers>, Computed Properties of 2127-03-9, the main research area is slipknotted protein folding optical tweezer direct observation.

Understanding the folding mechanism of knotted and slipknotted proteins has attracted considerable interest. Due to their topol. complexity, knotted and slipknotted proteins are predicted to fold slowly and involve large topol. barriers. Mol. dynamics simulation studies suggest that a slipknotted conformation can serve as an important intermediate to help greatly reduce the topol. difficulty during the folding of some knotted proteins. Here we use a single mol. optical tweezers technique to directly probe the folding of a small slipknotted protein AFV3-109. We found that stretching AFV3-109 can lead to the untying of the slipknot and complete unfolding of AFV3-109. Upon relaxation, AFV3-109 can readily refold back to its native slipknot conformation with high fidelity when the stretching force is lower than 6 pN. The refolding of AFV3-109 occurs in a sharp two-state like transition. Our results indicate that, different from knotted proteins, the folding of a slipknotted protein like AFV3-109 can be fast, and may not necessarily involve a high topol. barrier.

Nanoscale published new progress about Denaturation. 2127-03-9 belongs to class pyridine-derivatives, and the molecular formula is C10H8N2S2, Computed Properties of 2127-03-9.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Breitenbach, Benjamin B.; Steiert, Elena; Konhaeuser, Matthias; Vogt, Lea-Marie; Wang, Yujen; Parekh, Sapun H.; Wich, Peter R. published the artcile< Double stimuli-responsive polysaccharide block copolymers as green macrosurfactants for near-infrared photodynamic therapy>, Application In Synthesis of 2127-03-9, the main research area is polysaccharide copolymer surfactant photodynamic therapy nearinfrared radiation.

The NIR absorbing photosensitizer phthalocyanine zinc (PC(Zn)) was stabilized in aqueous media as water-dispersible nanoparticles with a reduction- and pH-responsive full polysaccharide block copolymer. A cellular uptake and also photo switchable intracellular activity of the cargo upon irradiation at wavelengths in the near IR region were shown. The block copolymer was synthesized by applying a copper-free click strategy based on a thiol exchange reaction, creating an amphiphilic double-stimuli-responsive mixed disulfide. The dual-sensitive polysaccharide micelles represent a non-toxic and biodegradable green macrosurfactant for the delivery of phthalocyanine zinc. By encapsulation into micellar nanoparticles, the bioavailability of PC(Zn) increased significantly, enabling smart photodynamic therapy for future applications in cancer-related diseases.

Soft Matter published new progress about Bioavailability. 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

Connon, Stephen J.; Hegarty, Anthony F. published the artcile< Stabilized 2,3-pyridyne reactive intermediates of exceptional dienophilicity>, Product Details of C6H5BrClNO, the main research area is regioselective lithiation thiophenoxy chloropyridine; thiophenoxy pyridyne preparation; pyridine endoxide preparation.

The enhanced dienophilicity of 4-methoxy, 4-aryloxy and 4-thiophenoxy analogs of 2,3-pyridyne relative to itself is reported. The regioselective lithiation of 4-alkoxy- and 4-thiophenoxy-2-chloropyridine at low temperatures, followed by elimination of lithium chloride affords 4-alkoxy- and 4-thiophenoxypyridynes, which can be trapped in situ in a [4+2] cycloaddition reaction with furan to give endoxides in moderate to good yields (25-58%). In contrast, precursors with a hydrogen or Me substituent at C-4 give no evidence for pyridyne formation under these conditions. Attempts to generate 6-isopropoxy-2,3-pyridyne from the low-temperature lithiation of 2-chloro-6-isopropoxypyridine were unsuccessful due to the instability of the 2-chloro-6-isopropoxy-5-lithiopyridine.

European Journal of Organic Chemistry published new progress about [4+2] Cycloaddition reaction. 777931-67-6 belongs to class pyridine-derivatives, and the molecular formula is C6H5BrClNO, Product Details of C6H5BrClNO.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Rai, Roopa; Kolesnikov, Aleksandr; Sprengeler, Paul A.; Torkelson, Steven; Ton, Tony; Katz, Bradley A.; Yu, Christine; Hendrix, John; Shrader, William D.; Stephens, Robin; Cabuslay, Ronnell; Sanford, Ellen; Young, Wendy B. published the artcile< Discovery of novel heterocyclic factor VIIa inhibitors>, Category: pyridine-derivatives, the main research area is aminopyrrolopyridine preparation factor VIIa inhibitor SAR.

Structure-activity relationships and binding mode of novel heterocyclic factor VIIa inhibitors will be described. In these inhibitors, a highly basic 5-amidinoindole moiety has been successfully replaced with a less basic 5-aminopyrrolo[3,2-b]pyridine scaffold.

Bioorganic & Medicinal Chemistry Letters published new progress about Anticoagulants. 220731-04-4 belongs to class pyridine-derivatives, and the molecular formula is C10H15N3O2, Category: pyridine-derivatives.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Jiang, Xiaoyue; Ye, Weidong; Song, Xiaohua; Ma, Wenxin; Lao, Xuejun; Shen, Runpu published the artcile< Novel ionic liquid with both Lewis and Bronsted acid sites for Michael addition>, Reference of 21876-43-7, the main research area is ionic liquid Lewis Bronsted acid preparation Michael addition; Lewis and Brønsted acid sites; Michael addition; novel ionic liquid.

Ionic liquid with both Lewis and Bronsted acid sites has been synthesized and its catalytic activities for Michael addition were carefully studied. The novel ionic liquid was stable to water and could be used in aqueous solution The molar ratio of the Lewis and Bronsted acid sites could be adjusted to match different reactions. The results showed that the novel ionic liquid was very efficient for a Michael addition and the synthesis of the target compounds was achieved in good to excellent yield within several min. Operational simplicity, high stability to water and air, small amount used, low cost of the catalyst used, high yields, chemoselectivity, applicability to large-scale reactions and reusability are the key features of this methodol., which indicated that this novel ionic liquid also holds great potential for environmentally friendly processes (green chem. methods).

International Journal of Molecular Sciences published new progress about Alkenes Role: RCT (Reactant), RACT (Reactant or Reagent). 21876-43-7 belongs to class pyridine-derivatives, and the molecular formula is C9H13NO3S, Reference of 21876-43-7.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Wu, Yue; Jiang, Zhensheng; Li, Zhihong; Gu, Jing; You, Qidong; Zhang, Xiaojin published the artcile< Click Chemistry-Based Discovery of [3-Hydroxy-5-(1H-1,2,3-triazol-4-yl)picolinoyl]glycines as Orally Active Hypoxia-Inducing Factor Prolyl Hydroxylase Inhibitors with Favorable Safety Profiles for the Treatment of Anemia>, Synthetic Route of 870997-85-6, the main research area is preparation hydroxytriazolyl picolinoyl glycine derivative HIF PHD2 inhibitor anemia.

As a gene associated with anemia, the erythropoiesis gene is physiol. expressed under hypoxia regulated by †hypoxia-inducing factor-α (HIF-α). Thus, stabilizing HIF-α is a potent strategy to stimulate the expression and secretion of erythropoiesis. In this study, we applied click chem. to the discovery of HIF prolyl hydroxylase 2 (HIF-PHD2) inhibitors for the first time, and a series of triazole compounds showed preferable inhibitory activity in fluorescence polarization assays. Of particular note was the orally active HIF-PHD inhibitor 15i (IC50 = 62.23 nM), which was almost ten times more active than the phase III drug FG-4592 (IC50 = 591.4 nM). Furthermore, it can upregulate the Hb of cisplatin-induced anemia mice (120 g/L) to normal levels (160 g/L) with no apparent toxicity observed in vivo. These results confirm that triazole compound 15i is a promising candidate for the treatment of renal anemia.

Journal of Medicinal Chemistry published new progress about Anemia. 870997-85-6 belongs to class pyridine-derivatives, and the molecular formula is C6H5BrN2O2, Synthetic Route of 870997-85-6.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Zhou, Bo; Wang, Yang; Yan, Yiwu; Mariscal, Javier; Di Vizio, Dolores; Freeman, Michael R.; Yang, Wei published the artcile< Low-Background Acyl-Biotinyl Exchange Largely Eliminates the Coisolation of Non-S-Acylated Proteins and Enables Deep S-Acylproteomic Analysis>, HPLC of Formula: 2127-03-9, the main research area is acyl biotinyl exchange S acylated protein proteomic.

Protein S-acylation (also called palmitoylation) is a common post-translational modification whose deregulation plays a key role in the pathogenesis of many diseases. Acyl-biotinyl exchange (ABE), a widely used method for the enrichment of S-acylated proteins, has the potential of capturing the entire S-acylproteome in any type of biol. sample. Here, we showed that current ABE methods suffer from a high background arising from the coisolation of non-S-acylated proteins. The background can be substantially reduced by an addnl. blockage of residual free cysteine residues with 2,2′-dithiodipyridine prior to the biotin-HPDP reaction. Coupling the low-background ABE (LB-ABE) method with label-free proteomics, 2 895 high-confidence candidate S-acylated proteins (including 1 591 known S-acylated proteins) were identified from human prostate cancer LNCaP cells, representing so-far the largest S-acylproteome data set identified in a single study. Immunoblotting anal. confirmed the S-acylation of five known and five novel prostate cancer-related S-acylated proteins in LNCaP cells and suggested that their S-acylation levels were about 0.6-1.8%. In summary, the LB-ABE method largely eliminates the coisolation of non-S-acylated proteins and enables deep S-acylproteomic anal. It is expected to facilitate a much more comprehensive and accurate quantification of S-acylproteomes than previous ABE methods.

Analytical Chemistry (Washington, DC, United States) published new progress about Mammalian cell. 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

Hansen-Felby, Magnus; Sommerfeldt, Andreas; Henriksen, Martin Lahn; Pedersen, Steen Uttrup; Daasbjerg, Kim published the artcile< Synthesis and depolymerization of self-immolative poly(disulfide)s with saturated aliphatic backbones>, Reference of 2127-03-9, the main research area is polydisulfide saturated aliphatic backbone depolymerization.

Self-immolative polymers (SIPs) are a class of degradable stimuli-responsive polymers, which, upon removal of labile end-caps, depolymerize selectively and stepwise to small mols. In light of our recent discovery of poly(dithiothreitol) (pDTT), a versatile SIP with a remarkably simple synthesis procedure, we investigated a broader range of unfunctionalized poly(disulfide)s. It is demonstrated that saturated aliphatic backbones can easily be made from 1,4-butanedithiol, 1,5-pentanedithiol, and 1,6-hexanedithiol monomers and, compared with pDTT, these polymers show enhanced stability, solubility, and processability. SIP polymers derived from the smaller 1,3-propanedithiol monomer with end-caps installed could not be synthesized. Polymers of 1,4-butanedithiol and 1,5-pentanedithiol undergo end-to-end depolymerizations upon end-cap removal, taking hours to days under basic conditions and not minutes as for pDTT. Degradation of the polymer of 1,6-hexanedithiol occurs by less well-defined pathways providing a complex product mixture of macrocyclic disulfides.

Polymer Chemistry published new progress about Crystallinity. 2127-03-9 belongs to class pyridine-derivatives, and the molecular formula is C10H8N2S2, Reference of 2127-03-9.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Potapov, Vladimir A.; Ishigeev, Roman S.; Amosova, Svetlana V.; Borodina, Tatyana N. published the artcile< Synthesis of a novel family of water-soluble 2H,3H-[1,3]thia- and -selenazolo[3,2-a]pyridin-4-ium heterocycles by annulation reactions>, Quality Control of 2127-03-9, the main research area is thia selenazolopyridinium heterocycle preparation annulation.

Regioselective synthesis of a novel family of water-soluble 2H,3H-[1,3]chalcogenazolo[3,2-a]pyridin-4-ium derivatives was developed based on 2-pyridinesulfenyl and -selenenyl halides and unsaturated compounds The annulation reactions with divinyl sulfide, selenide and N-vinylpyrrolidin-2-one led to addition of the chalcogen atom to the terminal carbon of the double bond whereas the reaction with tetravinylsilane proceeded with opposite regiochem. Tricyclic condensed heterocycles were obtained from 2,3-dihydrofuran and cycloalkenes. The products represent novel promising scaffolds for organic synthesis and possible drug discovery.

Tetrahedron Letters published new progress about Azoles Role: PRP (Properties), SPN (Synthetic Preparation), PREP (Preparation). 2127-03-9 belongs to class pyridine-derivatives, and the molecular formula is C10H8N2S2, Quality Control of 2127-03-9.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Willems, J. published the artcile< Aliphatic hydroxysulfonic acids and their internal esters: the sultones. II. The sultones>, Formula: C9H13NO3S, the main research area is .

CHR.(CH2)n.CHR’.SO2 (I) were prepared by concentration of an alc. solution of HOCHR(CH2)nCHR’SO3H (II) (from treating the Na salt in alc. with dry HCl) and distillation in vacuo (those of high mol. weight may decompose), by addition of Butyl Cellosolve (III) to the concentrated solution, distillation at 760 mm. until the b.p. (170°) of III is reached, and rectification in vacuo, and by addition of the alc. solution of II dropwise to boiling, stirred xylene (3 l. per mol), and the H2O distilled off as an azeotropic mixture of H2O-alc.-xylene until the b.p. of xylene is reached, the volume kept constant by dropwise addition of xylene, the solution cooled, washed with 2% NaHCO3 (important to keep from decomposition), and with H2O, dried, and the I obtained by distillation or precipitation with ligroine. The last method is generally applicable, simplest, and gives the best yields. The rate of reaction is not influenced by the pH, or by dehydrating agents. The reaction takes place near 150°, and not in low-boiling diluents, e.g. C6H6. 5- and 6-membered sultone rings are easily formed, and a 7-membered ring was obtained, but I could not be formed when n = 2 or 11. The following derivatives of I were prepared [R, n, R’, b.p./mm., m.p., d25, n25, M R, and m.p. of the corresponding pyridinoalkylsulfonic acid betaine (from boiling I in excess C5H5N), and its crystallizing solvent given]: H, 1, H (IV), 121°/1 (140°/8), 31°, -, -, -, 261°, alc.-H2O; H, 2, H (V), 153°/14, 15°, 1.3319, 1.4615, 28.15, 239°, isoamyl alc.; Me, 1, H (VI), 124°/2 (157.5°/14), -, 1.2929, 1.4500, 28.20, 240°, EtOH; H, 1, Me (VII), 124°/1.5, -, 1.3004, 1.4525, 28.24, 246°, MeOH; Me, 1, Me, 129°/1, -, 1.2220, 1.4511, 33.00, 270-71°, EtOH; H, 3, H (VIII), 155-6°/2, -, 1.2542, 1.4605, 32.65, 233-4°, EtOH; Me, 1, Pr (IX), 143-3.5°/4.2, -, 1.3359, 1.4520, 42.10, 230-32°, BuOH-Et2O; Bu, 1, H, 141°/2, -, -, -, -, 262-3°, EtOH-Et2O; Pr, 2, H, 126°/0.4, -, -, -, -, 263-4°, EtOH-Et2O; Me2CH(CH2)2, 1, H, 130°/1.5, -, -, -, -, 229-30°, absolute EtOH-Et2O; Me, 1, Me(CH2)5, 145°/0.6, -, -, -, -, 185°, EtOH-Et2O; Me(CH2)7, 1, H, 160-3°/0.5, -, -, -, -, 222.5-3.0°, BuOH; Me, 1, Me(CH2)13, -, half solid oil, -, -, -, 155°, EtOH/Et2O; Me(CH2)15, 1, H, -, 81° (EtOH), -, -, -, 214-15°, absolute EtOH; Me, 1, Ph, -, 106° (EtOH), -, -, -, 295-6.5°, EtOH-H2O. Also prepared were: O.CHMe.CH2.CMe2.SO2 (X), 160°/16, 50.5° (ligroine-Et2O), -, -, -, 253-4°, AmOH; O.CHMe.CHMe.CHPr.SO2, 128°/1.5, -, -, -, -, 245-6°, BuOH; O.CHMe.CHMe.CH[(CH2)5Me].SO2, 155°/1.5, -, -, -, -, -, – (C5H5N derivative very hygroscopic). Anilino sulfonic acids (PhNHCHRCH2CHR’SO3H) were prepared quant. by boiling equivalent amounts of PhNH2 and the following sultones 3-4 h. in C6H6 (m.p. of the PhNH derivative and crystallizing solvent given): IV, 248-9°, 90% EtOH; VI, 276-8°, H2O; VII, 254°, MeOH; X, 267-8°, EtOH; IX, 235.5-6°, BuOH. The reactions with PhNH2 and C5H5N show I to be alkylating agents, which provide a method for introducing the SO3 group and the attendant H2O solubility into certain compounds Also 1.g. IV mixed in a mortar with 1.09 g. p-H2NC6H4OH, the mixture heated 30 min. on the H2O bath, boiled with Me2CO to remove unreacted p-H2NC6H4OH, and crystallized from H2O, yielded 83% p-HOC6H4NH(CH2)3SO3H, m. 249°; 1.36 g. V boiled 6 h. in 25 cc. xylene with 1.29 g. octylamine gave Me(CH2)7NH(CH2)4SO3H.H2O, m. 172-3°. V (2.72 g.) with 2.88 g. β-naphthol in 0.8 g. NaOH solution precipitated immediately β-C10H7O(CH2)4CO3Na (beautiful crystals from EtOH-H2O). Similarly, VIII yielded 93% β-C10H7O(CH2)5SO3Na. The sultones keep their sulfoalkylating properties when reacting with RMgBr. V (13.6 g.) in absolute Et2O, dropped into Et2O containing EtMgBr (from 10.9 g. EtBr and 3 g. Mg) yielded 60% Me(CH2)5SO3K (phenylhydrazine salt, m. 101.5-2°, gave no depression of the m.p. of an authentic sample).

Bulletin des Societes Chimiques Belges published new progress about Lactones, sultones. 21876-43-7 belongs to class pyridine-derivatives, and the molecular formula is C9H13NO3S, Formula: C9H13NO3S.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem