Month: October 2022

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

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

Mizukawa, Yuki; Ikegami-Kawai, Mayumi; Horiuchi, Masako; Kaiser, Marcel; Kojima, Masayoshi; Sakanoue, Seiki; Miyagi, Seiya; Nanga Chick, Christian; Togashi, Hiroyuki; Tsubuki, Masayoshi; Ihara, Masataka; Usuki, Toyonobu; Itoh, Isamu published the artcile< Quest for a potent antimalarial drug lead: Synthesis and evaluation of 6,7-dimethoxyquinazoline-2,4-diamines>, Reference of 3731-53-1, the main research area is dimethoxyquinazolinediamine preparation antimalarial; Antimalarial drug; Derivatization; Quinazoline-2,4-diamines; SAR.

Quinazolines have long been known to exert varied pharmacol. activities that make them suitable for use in treating hypertension, viral infections, tumors, and malaria. Since 2014, author’s have synthesized approx. 150 different 6,7-dimethoxyquinazoline-2,4-diamines and evaluated their antimalarial activity via structure-activity relationship studies. Here, author’s summarize the results and report the discovery of 6,7-dimethoxy-N4-(1-phenylethyl)-2-(pyrrolidin-1-yl)quinazolin-4-amine, which exhibits high antimalarial activity as a promising antimalarial drug lead.

Bioorganic & 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, Reference of 3731-53-1.

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

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

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

Zhang, Guoqi; Cheng, Jessica; Davis, Kezia; Bonifacio, Mary Grace; Zajaczkowski, Cynthia published the artcile< Practical and selective hydroboration of aldehydes and ketones in air catalysed by an iron(II) coordination polymer>, Product Details of C7H7NO, the main research area is hydroboration aldehyde ketone green chem iron coordination polymer catalyst.

The in air catalytic hydroboration of ketones and aldehydes with pinacolborane by an iron(II) coordination polymer (CP) is carried out under mild and solvent-free conditions. The precatalyst is highly active towards a wide range of substrates including functionalized ketones and aldehydes in the presence of KOtBu as an activator, achieving a high turnover number (TON) of up to 9500. Excellent chemoselectivity to aldehydes over ketones was also revealed, which is in sharp contrast with the results obtained under inert atm. using the same catalyst system. This catalyst observed here is not only highly efficient but also recyclable for reuse for at least 5 times without losing its effectiveness.

Green Chemistry published new progress about Alcohols Role: SPN (Synthetic Preparation), PREP (Preparation). 350-03-8 belongs to class pyridine-derivatives, and the molecular formula is C7H7NO, Product Details of C7H7NO.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Duong, Thi-Mai Huong; Nobusue, Shunpei; Tada, Hirokazu published the artcile< Preparation of perovskite-derived one dimensional single crystals based on edge-shared octahedrons with pyridine derivatives>, HPLC of Formula: 3731-53-1, the main research area is lead pyridine derivative iodo complex perovskite preparation crystal structure; optical band gap lead pyridine derivative iodo complex perovskite.

Single crystals of hybrid materials based on 1D lead iodide perovskite networks with 2 pyridine (Py) derivatives, 4-Et (4Et)Py and 4-aminomethyl (4AM)Py, were prepared The compounds assembled into edge-shared lead iodide chains that formed needle-shaped crystals with lengths >1 cm. The crystal containing (4Et)Py formed in the triclinic system with P1 symmetry. The mols. were stacked along with the novel triple chain of 1D perovskite-derived networks. The crystal containing 4AMPy formed in the monoclinic system with P21/a symmetry. The amino group formed H bonds to I-. The optical band gaps for the 4EtPy-based and 4AMPy-based crystals are 2.73 eV and 2.64 eV, resp. The slight difference between the functional groups of the 2 mols. governed their crystal structures and hence optical properties.

Journal of Crystal Growth published new progress about Crystal structure. 3731-53-1 belongs to class pyridine-derivatives, and the molecular formula is C6H8N2, HPLC of Formula: 3731-53-1.

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