Month: November 2022

Kothandaraman, Shankaran; Donnely, Karla L.; Butora, Gabor; Jiao, Richard; Pasternak, Alexander; Morriello, Gregori J.; Goble, Stephen D.; Zhou, Changyou; Mills, Sander G.; MacCoss, Malcolm; Vicario, Pasquale P.; Ayala, Julia M.; DeMartino, Julie A.; Struthers, Mary; Cascieri, Margaret A.; Yang, Lihu published the artcile< Design, synthesis, and structure-activity relationship of novel CCR2 antagonists>, Reference of 112-63-0, the main research area is tetrahydropyranylaminocyclopentanecarboxamide preparation CCR2 antagonist.

A series of novel 1-aminocyclopentyl-3-carboxamides incorporating substituted tetrahydropyran moieties have been synthesized and evaluated for their antagonistic activity against the human CCR2 receptor. Among them analog I was found to posses potent antagonistic activity.

Bioorganic & Medicinal Chemistry Letters published new progress about CC chemokine receptor CCR2 Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 112-63-0 belongs to class esters-buliding-blocks, and the molecular formula is C19H34O2, Reference of 112-63-0.

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Hashemzadeh, Mehrnoosh; Movahed, Mohammad R.; Russu, Wade A.; Soroush, Ladan; Hill, Dine N. published the artcile< Novel design and synthesis of modified structure of carvedilol>, Reference of 112-63-0, the main research area is carvedilol analog synthesis beta blocker drug design heart failure.

β-Adrenergic blocking agents have been in use for nearly 40 years. β-Blockers have been more thoroughly studied in the past twenty years as they have become commonly prescribed to heart failure patients. The class of β-blockers has grown considerably and has many pharmaceutical applications in patients with heart failure. Carvedilol has been the most effective beta-blocker in the treatment of the systolic heart failure. Carvedilol is a non-selective β- and α-blocker enantiomer with antioxidant effects that are attributed to its carbazole moiety. Carvedilol is taken twice daily because it is extensively metabolized and therefore loses its effectiveness due to a short half-life. Recently a long acting carvedilol has become available, as Coreg CR. Coreg CR is available for once-a-day administration as controlled-release oral capsules containing 10, 20, 40, or 80 mg carvedilol phosphate. The subject of the current report is to design a new structural analog of carvedilol that incorporates a protecting group such as a fluorine atom at position 8 of the carbazole ring for the purpose of blocking a critical metabolic pathway thus increasing its half life. This will follow discussion regarding current carvedilol patents. We believe that carvedilol activity will remain unchanged. The synthesis of 8-Fluoro-1, 2, 3, 9- tetrahydro-4H-carbazol-4-one, a key synthetic intermediate of the designed carvedilol analog, was carried out and successfully characterized.

Recent Patents on Cardiovascular Drug Discovery published new progress about Antioxidants. 112-63-0 belongs to class esters-buliding-blocks, and the molecular formula is C19H34O2, Reference of 112-63-0.

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Huang, Jiayi; Cui, Yahua; Yang, Yanling; Li, Huahua; Zhang, Yi; Yang, Haiju; Du, Shouying; Bai, Jie published the artcile< Optical Coherence Tomography and Microdialysis for Microneedle-Mediated Penetration Enhancement Study of Paeoniflorin-Loaded Ethosomes>, Reference of 112-63-0, the main research area is microneedle penetration paeoniflorin ethosome; Ethosome; Microdialysis; Microneedle; Optical coherence tomography; Pharmacokinetics.

This paper uses microdialysis to systematically study the percutaneous pharmacokinetics of paeoniflorin-loaded ethosomes. First, optical coherence tomog. (OCT) was used to study the effectiveness of microneedle puncture. Second, a microdialysis method and a UPLC-MS method for determining the amount of paeoniflorin (Pae) in dialyzate were established. Finally, the transdermal pharmacokinetics of TGP-E was studied using in vivo microdialysis in rats under the above MN-assisted conditions. The optimal MN-assisted conditions were obtained at a microneedle length of 500μm, a pressure of 3 N, and an action time of 3 min. The pharmacokinetic results demonstrated that the maximum drug concentration (Cmax) and the area under the curve (AUC) of the TGP-E gel were higher than the TGP-saline solution gel, and the mean retention time was lower. These indicated that microneedle can promote the entry of the ethosomes into the skin for in vivo experiments and greatly improve the possibility of deep penetration of the water-soluble Pae. Therefore, the microneedle-ethosomes delivery system is a more ideal means for promoting the deep penetration of Pae. These findings may provide a reference for the combination of multiple penetration-enhancement ways to promote drug absorption, and also provide a new insight to realize the development of novel, safe, and more effective dosage forms and administration routes of drugs.

Skin Pharmacology and Physiology published new progress about Absorption. 112-63-0 belongs to class esters-buliding-blocks, and the molecular formula is C19H34O2, Reference of 112-63-0.

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Guan, Ting; Guo, Jing-Yu; Zhang, Qing-Hong; Xu, Xin-Wen; Yu, Xiao-Yu; Zhang, Yu; Zhao, Kai published the artcile< Photoredox-catalyzed regio- & stereoselective C(sp2)-H cyanoalkylation of enamides with cycloketone oximes via selective C-C bond cleavage/radical addition cascade>, Safety of (9Z,12Z)-Methyl octadeca-9,12-dienoate, the main research area is cyanoalkyl enamide preparation regioselective diastereoselective green chem; enamide cycloketone oxime Heck type cyanoalkylation photoredox catalyst.

A photoredox-catalyzed regio- and stereoselective Heck-type cyanoalkylation of synthetically prominent enamides R1C(=CH2)N(R2)(R3) (R1 = Ph, thiophen-3-yl, 2H-1,3-benzodioxol-5-yl, etc.; R2 = Ac, Bn; R3 = Bn, Me, cyclohexylmethyl, etc.) with cycloketone oximes I (Y = CH, N; R4 = H, n-C6H13, cyclohexylmethyl, Bn, etc.; R5 = H, Ph, CN, Boc, etc.; n = 1, 2) via selective β-C-C bond scission/selective radical addition cascade is developed, enabling the incorporation of synthetically versatile and pharmaceutically appealing distal cyanoalkyl moieties into enamide scaffolds R1C(N(R2)(R3))=CHCH(R4)Y(R5)(CH2)nCN under mild conditions. The synthetic importance of this methodol. was highlighted by the broad substrate scopes, satisfying functional group compatibilities, excellent regio- and stereoselectivities as well as the versatile and diverse synthetic applications of β-cyanoalkylated enamides.

Green Chemistry published new progress about Aliphatic nitriles Role: PRP (Properties), RCT (Reactant), SPN (Synthetic Preparation), RACT (Reactant or Reagent), PREP (Preparation). 112-63-0 belongs to class esters-buliding-blocks, and the molecular formula is C19H34O2, Safety of (9Z,12Z)-Methyl octadeca-9,12-dienoate.

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Gilmour, Sandra; Marder, Seth R.; Tiemann, Bruce G.; Cheng, Lap Tak published the artcile< Synthesis and first hyperpolarizabilities of acceptor-substituted β-apo-8'-carotenal derived compounds>, Related Products of 112-63-0, the main research area is hyperpolarizability apocarotenal derivative; optical property apocarotenal derivative; harmonic generation apocarotenal derivative.

The synthesis and second-order nonlinear optical properties of acceptor-substituted biol. derived β-apo-8′-carotenal compounds I [Z = C(CN)2, (E)-CHC6H4NO2-4] are reported. Elec. field-induced second harmonic generation (EFISH) measurements give values of β(0) which are 2-6 times greater than for 4-N,N-dimethylamino-4′-nitrostilbene (DANS).

Journal of the Chemical Society, Chemical Communications published new progress about Carotenes Role: SPN (Synthetic Preparation), PREP (Preparation). 112-63-0 belongs to class esters-buliding-blocks, and the molecular formula is C19H34O2, Related Products of 112-63-0.

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Ali, Mohammed Hashmat; Stricklin, Susan published the artcile< Oxidation of sulfides with pyridinium tribromide in the presence of hydrated silica gel>, COA of Formula: C19H34O2, the main research area is sulfide oxidation pyridinium bromide; sulfoxide preparation.

A variety of sulfides were oxidized to sulfoxides utilizing pyridinium tribromide in the presence of hydrated silica gel in a non-aqueous media. A combination of pyridinium tribromide and hydrated silica gel releases mol. bromine slowly in the reaction, affecting the oxidation Hydrated silica gel also promotes decomposition of the bromosulfonium intermediate to the product. This procedure employs non-aqueous media for the first time in such a reaction.

Synthetic Communications published new progress about Oxidation. 112-63-0 belongs to class esters-buliding-blocks, and the molecular formula is C19H34O2, COA of Formula: C19H34O2.

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Berger, Dan M.; Torres, Nancy; Dutia, Minu; Powell, Dennis; Ciszewski, Greg; Gopalsamy, Ariamala; Levin, Jeremy I.; Kim, Kyung-Hee; Xu, Weixin; Wilhelm, James; Hu, YongBo; Collins, Karen; Feldberg, Larry; Kim, Steven; Frommer, Eileen; Wojciechowicz, Donald; Mallon, Robert published the artcile< Non-hinge-binding pyrazolo[1,5-a]pyrimidines as potent B-Raf kinase inhibitors>, SDS of cas: 112-63-0, the main research area is pyrazolopyrimidine preparation BRaf kinase inhibitor.

As part of our research effort to discover B-Raf kinase inhibitors, we prepared a series of C-3 substituted N-(3-(pyrazolo[1,5-a]pyrimidin-7-yl)phenyl)-3-(trifluoromethyl)benzamides. X-ray crystallog. studies revealed that one of the more potent inhibitors bound to B-Raf kinase without forming a hinge-binding hydrogen bond. With basic amine residues appended to C-3 aryl residues, cellular activity and solubility were enhanced over previously described compounds of this class.

Bioorganic & Medicinal Chemistry Letters published new progress about Structure-activity relationship (B-Raf kinase-inhibiting). 112-63-0 belongs to class esters-buliding-blocks, and the molecular formula is C19H34O2, SDS of cas: 112-63-0.

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Zaleskaya-Hernik, Marta; Dobrzycki, Lukasz; Karbarz, Marcin; Romanski, Jan published the artcile< Fluorescence Recognition of Anions Using a Heteroditopic Receptor: Homogenous and Two-Phase Sensing>, Product Details of C19H34O2, the main research area is crown ether squaramide ion pair receptor fluorescent sensor; anthracene; crown ethers; fluorescent sensors; ion pair receptors; squaramides; sulfate extraction.

In contrast to monotopic receptor 3, the anthracene functionalized squaramide dual-host receptor 1 is capable of selectively extracting sulfate salts, as was evidenced unambiguously by DOSY, mass spectrometry, fluorescent and ion chromatog. measurements. The receptors were investigated in terms of anion and ion pair binding using the UV-vis and 1H NMR titrations method in acetonitrile. The reference anion receptor 3, lacking a crown ether unit, was found to lose the enhancement in anion binding induced by the presence of cations. Besides the ability to bind anions in an enhanced manner exhibited by ion pair receptors 2 and 4, changing the 1-aminoanthracene substituent resulted in their exhibiting a lower anion affinity than receptor 1. By using receptor 1 and adjusting the water content in organic phase it was possible to selectively detect sulfates both by “”turn-off”” and “”turn-on”” fluorescence, and to do so homogenously and under interfacial conditions. Such properties of receptor 1 have allowed the development of a new type of sensor capable of recognizing and extracting potassium sulfate from the aqueous medium across a phase boundary, resulting in an appropriate fluorescent response in the organic solution

International Journal of Molecular Sciences published new progress about Aqueous solutions. 112-63-0 belongs to class esters-buliding-blocks, and the molecular formula is C19H34O2, Product Details of C19H34O2.

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Yang, Qin; Yin, Zheng-Lan; Ouyang, Ban-Lai; Peng, Yi-Yuan published the artcile< Pyridinium tribromide catalyzed condensation of indoles and aldehydes to form bisindolylalkanes>, Category: esters-buliding-blocks, the main research area is indole carbonyl aldehyde ketone condensation pyridinium bromide catalyst; alkane bisindolyl preparation.

An efficient synthetic method for bis(indol-3-yl)alkane derivatives was developed. In the presence of 5 mol% of pyridinium tribromide, the condensation of indoles and aldehydes proceeded smoothly under mild conditions, giving rise to the corresponding bis(indol-3-yl)alkanes in good to excellent yields.

Chinese Chemical Letters published new progress about Aldehydes Role: RCT (Reactant), RACT (Reactant or Reagent). 112-63-0 belongs to class esters-buliding-blocks, and the molecular formula is C19H34O2, Category: esters-buliding-blocks.

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Fan, Pei-Ru; Zhao, Xue; Wei, Ze-Hui; Huang, Yan-Ping; Liu, Zhao-Sheng published the artcile< Robust immobilized enzyme reactor based on trimethylolpropane trimethacrylate organic monolithic matrix through ""thiol-ene"" click reaction>, Application In Synthesis of 3290-92-4, the main research area is immobilized enzyme reactor trimethylolpropane trimethacrylate organic monolithic matrix.

A novel immobilized enzyme reactor (IMER) based on trimethylolpropane trimethacrylate (TRIM) organic monolith was prepared by “”thiol-ene”” click reaction. The IMERs were made by fabricating TRIM monolith core in advance. There were residual double bonds on the surface of TRIM monolith, in which click reaction can be performed with the free thiol groups of trypsin at room temperature to bond the trypsin on the monolithic column without addnl. introducing an active functional group. The enzyme activity was characterized by kinetic parameters Km and Vmax and determined by off-line chromatog. The performance of the IMERs was evaluated by digesting standard protein BSA and compared with in-solution digestion method. By using IMER 5 min, the sequence coverage rate of BSA was 79.41%, which was similar to that in-solution digestion for 12 h (82.7%). The applicability of the IMERs in complex samples was assessed by digesting crude protein extracts from egg white and mouse liver, identifying 28 (104 peptides) and 843 (3916 peptides) proteins, resp. All results indicated that the IMERs have great potential in high-throughput proteomics anal.

European Polymer Journal published new progress about Bioreactors. 3290-92-4 belongs to class esters-buliding-blocks, and the molecular formula is C18H26O6, Application In Synthesis of 3290-92-4.

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics