Tag: M.W=200-250

Kalliokoski, Tuomo; Rummakko, Petteri; Rantanen, Marja; Blaesse, Michael; Augustin, Martin; Ummenthala, Goverdhan Reddy; Choudhary, Sapan; Venalainen, Jarkko published the artcile< Discovery of sulfonamides and 9-oxo-2,8-diazaspiro[5,5]undecane-2-carboxamides as human kynurenine aminotransferase 2 (KAT2) inhibitors>, Application In Synthesis of 91419-53-3, the main research area is human kynurenine aminotransferase 2 KAT2 reversible inhibitor virtual screening; Human kynurenine aminotransferase 2; KAT2; Reversible inhibitor; Virtual screening.

Human kynurenine aminotransferase 2 (KAT2) inhibitors could be potentially used to treat the cognitive deficits associated with bipolar disease and schizophrenia. Although, there has been active drug research activity by several industrial and academic groups in developing KAT2 inhibitors over the years, no such compound has proceeded to the clinics. Here, we report two different chem. series of reversible KAT2 inhibitors with sub-micromolar activities. The first series was identified by a high-throughput screening of a diverse random library and the second one by structure-based virtual screening. Two novel crystal structures of KAT2 complexed with different reversible inhibitors were also deposited to the Protein databank which could be useful for future drug discovery efforts.

Bioorganic & Medicinal Chemistry Letters published new progress about Bipolar disorder. 91419-53-3 belongs to class piperidines, and the molecular formula is C11H18N2O2, Application In Synthesis of 91419-53-3.

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Blahun, Oleksandr P.; Melnychenko, Heorhii; Kuchkovska, Yuliya O.; Zhersh, Serhii; Tolmachev, Andrey A.; Grygorenko, Oleksandr O. published the artcile< Synthesis of Functionalized Bridged Bicyclic Sulfonamides with a Bridgehead Nitrogen Atom>, Recommanded Product: tert-Butyl 3-cyanopiperidine-1-carboxylate, the main research area is dioxothiazabicycloalkanecarboxylate bridged sultam preparation.

Sultams with bridgehead nitrogen atoms such as I and II were prepared Dioxothiazabicycloalkanecarboxylic acids such as I with carboxylic acid-substituted bridgehead atoms were prepared in seven steps from Boc-protected azaheterocyclylcarbonitriles such as tert-Bu 3-cyano-1-pyrrolidinecarboxylate by chloromethylation, substitution with a thiolate, oxidative chlorination, substitution of the sulfonyl chloride with fluoride, Boc deprotection, base-mediated cyclization, and nitrile hydrolysis. Dioxothiazabicycloalkanecarboxylic acids such as I with carboxylic acid-substituted bridging atoms were prepared by carboxylation of bridged sultams [prepared in six steps by literature procedures from Boc-protected (hydroxymethyl)azacycles]. Two approaches to the synthesis of functionalized bridged bicyclic sulfonamides with a bridgehead nitrogen atom were developed. Both types of bridged sultams were prepared on > 1g scales.

European Journal of Organic Chemistry published new progress about Carboxylation. 91419-53-3 belongs to class piperidines, and the molecular formula is C11H18N2O2, Recommanded Product: tert-Butyl 3-cyanopiperidine-1-carboxylate.

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Yu, Tao; Tagat, Jayaram R.; Kerekes, Angela D.; Doll, Ronald J.; Zhang, Yonglian; Xiao, Yushi; Esposite, Sara; Belanger, David B.; Curran, Patrick J.; Mandal, Amit K.; Siddiqui, M. Arshad; Shih, Neng-Yang; Basso, Andrea D.; Liu, Ming; Gray, Kimberly; Tevar, Seema; Jones, Jennifer; Lee, Suining; Liang, Lianzhu; Ponery, Samad; Smith, Elizabeth B.; Hruza, Alan; Voigt, Johannes; Ramanathan, Lata; Prosise, Winifred; Hu, Mengwei published the artcile< Discovery of a Potent, Injectable Inhibitor of Aurora Kinases Based on the Imidazo-[1,2-a]-Pyrazine Core>, Product Details of C11H18N2O2, the main research area is imidazopyrazine pyrazolyl isothiazolylamino derivative preparation aurora kinase inhibition activity; pyrazolyl isothiazolylamino imidazopyrazine solubility antitumor activity; Aurora kinase inhibitors; SCH 1473759; aqueous solubility; cell potency; imidazo-[1,2-a]-pyrazine; tumor xenograft model.

The imidazo-[1,2-a]-pyrazine I is a dual inhibitor of Aurora kinases A and B with modest cell potency (IC50 = 250 nM) and low solubility (5 μM). Lead optimization guided by the binding mode led to the acyclic amino alc. II (SCH 1473759), which is a picomolar inhibitor of Aurora kinases (TdF Kd Aur A = 0.02 nM and Aur B = 0.03 nM) with improved cell potency (phos-HH3 inhibition IC50 = 25 nM) and intrinsic aqueous solubility (11.4 mM). It also demonstrated efficacy and target engagement in human tumor xenograft mouse models.

ACS Medicinal Chemistry Letters published new progress about Antitumor agents. 91419-53-3 belongs to class piperidines, and the molecular formula is C11H18N2O2, Product Details of C11H18N2O2.

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Gross, Kathleen M. Bertini; Beak, Peter published the artcile< Complex-Induced Proximity Effects: The Effect of Varying Directing-Group Orientation on Carbamate-Directed Lithiation Reactions>, SDS of cas: 149518-50-3, the main research area is proximity effect complex induced; carbamate directed lithiation.

A series of selected bicyclic carbamates in which the range of accessible angles and distances between the carbonyl group and the proton removed in an α-lithiation reaction are structurally defined have been investigated. Oxazolidinones I (n = 1, 2; R = i-Pr, t-Bu) undergo stereoselective lithiation-substitution reactions to provide cis-II as the major diastereomers. Two series of competition experiments show that the conformationally restricted carbamates undergo lithiation via complexes more efficiently than Boc amines (e.g., N-Boc-pyrrolidine, N-Boc-piperidine). These results along with semiempirical calculations suggest that a small dihedral angle and a calculated distance of 2.78 Å between the carbamate carbonyl oxygen and the proton to be removed are favorable for a carbamate-directed lithiation. A series of tin-lithium exchange experiments indicate that the configurational stability of a carbamate-stabilized organolithium species may be enhanced by restrictive geometry.

Journal of the American Chemical Societypublished new progress about Chelation (and configurational stability of carbanion intermediate). 149518-50-3 belongs to class piperidines, and the molecular formula is C12H21NO4, SDS of cas: 149518-50-3.

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Nakajima, Noriyuki; Ubukata, Makoto published the artcile< Preparation of nitriles from primary amides under Swern oxidation conditions>, Synthetic Route of 91419-53-3, the main research area is Swern oxidation carboxamide; nitrile preparation.

In order to establish a mild conversion method of primary amides to nitriles, various types of carboxamides were treated under Swern oxidation conditions, (COCl)2-DMSO and Et3N, as a dehydrating agent to obtain desired nitriles in 75-96% yields.

Tetrahedron Letterspublished new progress about Amides Role: RCT (Reactant), RACT (Reactant or Reagent). 91419-53-3 belongs to class piperidines, and the molecular formula is C11H18N2O2, Synthetic Route of 91419-53-3.

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Liu, Richard Y.; Bae, Minwoo; Buchwald, Stephen L. published the artcile< Mechanistic Insight Facilitates Discovery of a Mild and Efficient Copper-Catalyzed Dehydration of Primary Amides to Nitriles Using Hydrosilanes>, Name: tert-Butyl 3-cyanopiperidine-1-carboxylate, the main research area is copper catalyst dehydration primary amide hydrosilane; nitrile preparation.

Metal-catalyzed silylative dehydration of primary amides is an economical approach to the synthesis of nitriles. A copper-hydride(CuH)-catalyzed process is reported that avoids a typically challenging 1,2-siloxane elimination step, thereby dramatically increasing the rate of the overall transformation relative to alternative metal-catalyzed systems. This new reaction proceeds at ambient temperature, tolerates a variety of metal-, acid-, or base-sensitive functional groups and can be performed using a simple ligand, inexpensive siloxanes and low catalyst loading.

Journal of the American Chemical Societypublished new progress about Amides Role: RCT (Reactant), SPN (Synthetic Preparation), RACT (Reactant or Reagent), PREP (Preparation). 91419-53-3 belongs to class piperidines, and the molecular formula is C11H18N2O2, Name: tert-Butyl 3-cyanopiperidine-1-carboxylate.

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Piperidine the name comes from the genus name Piper, which is the Latin word for pepper. 84358-13-4, formula is C11H19NO4, Name is 1-(tert-Butoxycarbonyl)piperidine-4-carboxylic acid. Although piperidine is a common organic compound, it is best known as a representative structure element within many pharmaceuticals and alkaloids, such as natural-occurring solenopsins. Category: piperidines.

Zhang, Ziyi;Chen, Zhiguo;Zhang, Shengyu;Shao, Xiao;Zhou, Zhiwen research published 《 Antibacterial activity of the structurally novel ocotillol-type lactone and its analogues》, the research content is summarized as follows. A novel series of ocotillol-type lactone derivatives were designed and synthesized in order to study their antibacterial activity and structure-activity relationships. Among which, compounds 4j and 4 m were found to be the most active with min. inhibitory concentrations (MICs) of 1-4 μg/mL against Gram-pos. bacteria and showed low cytotoxicity against MCF-7, HEK-293 and HK-2 cells at their MICs. The antibacterial effect of compound 4 m was characterized further by SEM, cytoplasmic β-galactosidase leakage assay and UV-visible anal. The results showed that 4 m may exert its antibacterial effect by damaging bacterial cell membranes and disrupting the function of DNA, both of which could lead to rapid cell death.

84358-13-4, N-BOC-piperidine-4-carboxylic acid, also known asN-Boc-isonipecotic acid , is a useful research compound. Its molecular formula is C11H19NO4 and its molecular weight is 229,28 g/mole. The purity is usually 95%.

N-Boc-isonipecotic acid is a potent antitumor agent that has been clinically shown to be effective against leukemia and lymphoma. It has potent antibacterial activity against Gram-positive bacteria such as Staphylococcus aureus and Streptococcus pyogenes. N-Boc-isonipecotic acid binds to the gyrase enzyme, which is used by these bacteria to maintain the integrity of their DNA, inhibiting protein synthesis and cell division. This drug also has anti-inflammatory properties. N-Boc-isonipecotic acid inhibits prostaglandin synthesis in cells, which may be due to its ability to inhibit the production of tumor necrosis factor α (TNFα) in macrophages., Category: piperidines

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Piperidine structural motif is present in numerous natural alkaloids. These include piperine, which gives black pepper its spicy taste. This gave the compound its name. 84358-13-4, formula is C11H19NO4, Name is 1-(tert-Butoxycarbonyl)piperidine-4-carboxylic acid. Other examples are the fire ant toxin solenopsin, the nicotine analog anabasine of tree tobacco (Nicotiana glauca), lobeline of Indian tobacco. Application of C11H19NO4.

Zhao, Haoqiang;Xu, Xin;Yu, Haiyang;Li, Bohan;Xu, Xingyu;Li, Huanrong;Xu, Lijin;Fan, Qinghua;Walsh, Patrick J. research published 《 Rh(I)-Catalyzed C6-Selective Decarbonylative Alkylation of 2-Pyridones with Alkyl Carboxylic Acids and Anhydrides》, the research content is summarized as follows. A Rh-catalyzed chelation-assisted C6-selective C-H activation/alkylation of 2-pyridones e.g., 1-(pyridin-2-yl)-1,2-dihydropyridin-2-one with readily available anhydrides RC(O)OC(O)R (R = Me, Et, 2-methylpropyl, etc.) or alkyl carboxylic acids R¹C(O)OH (R¹ = nonyl, cyanoethyl, cyclohexyl, etc.) is introduced. The reaction proceeds via substrate decarbonylation. This approach merges C-H functionalization with readily available anhydrides, allowing for the efficient synthesis of various C6-alkylated 2-pyridones e.g., 6-methyl-2H-[1,2′-bipyridin]-2-one with good functional group tolerance.

84358-13-4, N-BOC-piperidine-4-carboxylic acid, also known asN-Boc-isonipecotic acid , is a useful research compound. Its molecular formula is C11H19NO4 and its molecular weight is 229,28 g/mole. The purity is usually 95%.

N-Boc-isonipecotic acid is a potent antitumor agent that has been clinically shown to be effective against leukemia and lymphoma. It has potent antibacterial activity against Gram-positive bacteria such as Staphylococcus aureus and Streptococcus pyogenes. N-Boc-isonipecotic acid binds to the gyrase enzyme, which is used by these bacteria to maintain the integrity of their DNA, inhibiting protein synthesis and cell division. This drug also has anti-inflammatory properties. N-Boc-isonipecotic acid inhibits prostaglandin synthesis in cells, which may be due to its ability to inhibit the production of tumor necrosis factor α (TNFα) in macrophages., Application of C11H19NO4

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Piperidine was first reported in 1850 by the Scottish chemist Thomas Anderson and again, independently, in 1852 by the French chemist 84358-13-4, formula is C11H19NO4, Name is 1-(tert-Butoxycarbonyl)piperidine-4-carboxylic acid. Auguste Cahours, who named it. Both of them obtained piperidine by reacting piperine with nitric acid. Quality Control of 84358-13-4.

Zhao, Yanmei;Xu, Lei;Zhang, Jiankang;Zhang, Mengmeng;Lu, Jingyi;He, Ruoyu;Xi, Jianjun;Zhuang, Rangxiao;Li, Jia;Zhou, Yubo research published 《 Optimization of piperidine constructed peptidyl derivatives as proteasome inhibitors》, the research content is summarized as follows. A series of non-covalent piperidine-containing peptidyl derivatives with various substituents at side chains of different residues were designed, synthesized and evaluated as proteasome inhibitors. After proteasome inhibitory evaluations of all the synthesized target compounds, selected ones were tested for their anti-proliferation activities against three multiple myeloma (MM) cell lines. Eight analogs displayed more potent activities than carfilzomib, and the most promising compound 24 (I) showed IC₅₀ values of 0.8 ± 0.2 nM against 20S proteasome and 8.42 ± 0.74 nM, 7.14 ± 0.52 nM, 14.20 ± 1.08 nM for RPMI 8226, NCI-H929 and MM.1S cell lines, resp. Addnl., mechanisms of anti-cancer activity of representative compound 24 were further investigated. Apoptosis of RPMI-8226 cells were achieved through accumulating polyubiquitin and inducing the cleavage of caspase and PARP. Besides, half-life in rat plasma of compound 24 was prolonged after optimization, which would be helpful for increasing in vivo activities of this series of derivatives All the studies confirmed that piperidine-containing non-covalent proteasome inhibitors can be potential leads for anti-MM drug development.

84358-13-4, N-BOC-piperidine-4-carboxylic acid, also known asN-Boc-isonipecotic acid , is a useful research compound. Its molecular formula is C11H19NO4 and its molecular weight is 229,28 g/mole. The purity is usually 95%.

N-Boc-isonipecotic acid is a potent antitumor agent that has been clinically shown to be effective against leukemia and lymphoma. It has potent antibacterial activity against Gram-positive bacteria such as Staphylococcus aureus and Streptococcus pyogenes. N-Boc-isonipecotic acid binds to the gyrase enzyme, which is used by these bacteria to maintain the integrity of their DNA, inhibiting protein synthesis and cell division. This drug also has anti-inflammatory properties. N-Boc-isonipecotic acid inhibits prostaglandin synthesis in cells, which may be due to its ability to inhibit the production of tumor necrosis factor α (TNFα) in macrophages., Quality Control of 84358-13-4

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Industrially, piperidine is produced by the hydrogenation of pyridine, usually over a molybdenum disulfide catalyst: C5H5N + 3 H2 → C5H10NH. 84358-13-4, formula is C11H19NO4, Name is 1-(tert-Butoxycarbonyl)piperidine-4-carboxylic acid. Pyridine can also be reduced to piperidine via a modified Birch reduction using sodium in ethanol. Product Details of C11H19NO4.

Zhi, Zhuoer;Zhang, Wenting;Yao, Jingchun;Shang, Yanguo;Hao, Qingjing;Liu, Zhong;Ren, Yushan;Li, Jie;Zhang, Guimin;Wang, Jinxin research published 《 Discovery of Aryl Formyl Piperidine Derivatives as Potent, Reversible, and Selective Monoacylglycerol Lipase Inhibitors》, the research content is summarized as follows. Most of the current MAGL inhibitors function by an irreversible mechanism of action, causing a series of side effects. Herein, starting from irreversible inhibitors, 25 compounds were synthesized and evaluated in vitro for MAGL inhibition, among which, compound I showed the most potent inhibitory activity (IC50 = 15 nM). Crucially, docking studies demonstrated that the m-chlorine-substituted aniline fragment occupied a hydrophobic sub-pocket enclosed by side chains of Val191, Tyr194, Val270, and Lys273, which creatively identify a new key anchoring point for the development of new MAGL inhibitors. Furthermore, in vivo evaluation innovatively revealed that this reversible inhibitor I significantly displayed the depressive-like behaviors induced by reserpine. To the best of our knowledge, this is the first time that reversible inhibitors of MAGL were developed to support MAGL as a potential therapeutic target for depression.

Product Details of C11H19NO4, N-BOC-piperidine-4-carboxylic acid, also known asN-Boc-isonipecotic acid , is a useful research compound. Its molecular formula is C11H19NO4 and its molecular weight is 229,28 g/mole. The purity is usually 95%.

N-Boc-isonipecotic acid is a potent antitumor agent that has been clinically shown to be effective against leukemia and lymphoma. It has potent antibacterial activity against Gram-positive bacteria such as Staphylococcus aureus and Streptococcus pyogenes. N-Boc-isonipecotic acid binds to the gyrase enzyme, which is used by these bacteria to maintain the integrity of their DNA, inhibiting protein synthesis and cell division. This drug also has anti-inflammatory properties. N-Boc-isonipecotic acid inhibits prostaglandin synthesis in cells, which may be due to its ability to inhibit the production of tumor necrosis factor α (TNFα) in macrophages., 84358-13-4.

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem