Tag: 300-400

On July 31, 2021, Owen, Benjamin; Bichler, Edyta; Benveniste, Morris published an article.Name: 2-Ethylhexyl 2-cyano-3,3-diphenylacrylate The title of the article was Excitatory synaptic transmission in hippocampal area CA1 is enhanced then reduced as chronic epilepsy progresses. And the article contained the following:

This study examines changes in synaptic transmission with progression of the chronic epileptic state. Male Sprague-Dawley rats (P40-45) were injected with either saline or pilocarpine. In rats injected with pilocarpine, status epilepticus ensued. Hippocampal slices were cut 20-60 days or 80-110 days post-treatment. Evoked and miniature EPSCs (mEPSCs) were recorded from CA1 pyramidal neurons using whole-cell voltage-clamp. Fiber volleys were also recorded from stratum radiatum. Evoked EPSCs from the pilocarpine-treated cohort showed enhanced amplitudes 20-60 days post-treatment compared to the saline-treated cohort, whereas mEPSCs recorded from the same age group showed no change in event frequency and a slight but significant decrease in mEPSC amplitude distribution. In contrast, comparing evoked EPSCs and mEPSCs recorded 80-110 days after treatment indicated reduced amplitudes from pilocarpine-treated animals compared to controls. mEPSC inter-event interval decreased. This could be explained by a partial depletion of the ready releasable pool of neurotransmitter vesicles in Schaffer collateral presynaptic terminals of the pilocarpine-treated rats. In both saline- and pilocarpine-treated cohorts, concomitant decreases in mEPSC amplitudes as time after treatment progressed suggest that age-related changes in CA1 circuitry may be partially responsible for changes in synaptic transmission that may influence the chronic epileptic state. The experimental process involved the reaction of 2-Ethylhexyl 2-cyano-3,3-diphenylacrylate(cas: 6197-30-4).Name: 2-Ethylhexyl 2-cyano-3,3-diphenylacrylate

The Article related to pilocarpine ca1 antiepilepsy agent chronic epilepsy, aging, epscs, epilepsy, fiber volleys, hippocampus, pilocarpine, status epilepticus, synaptic transmission, mepscs, Pharmacology: Effects Of Nervous System- and Behavior-Affecting Drugs and Neuromuscular Agents and other aspects.Name: 2-Ethylhexyl 2-cyano-3,3-diphenylacrylate

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

On June 30, 2021, Coppi, Elisabetta; Buonvicino, Daniela; Ranieri, Giuseppe; Cherchi, Federica; Venturini, Martina; Pugliese, Anna Maria; Chiarugi, Alberto published an article.Name: 2-Ethylhexyl 2-cyano-3,3-diphenylacrylate The title of the article was Dexpramipexole Enhances K+ Currents and Inhibits Cell Excitability in the Rat Hippocampus In Vitro. And the article contained the following:

Dexpramipexole (DEX) has been described as the first-in-class F1Fo ATP synthase activator able to boost mitochondrial bioenergetics and provide neuroprotection in exptl. models of ischemic brain injury. Although DEX failed in a phase III trial in patients with amyotrophic lateral sclerosis, it showed favorable safety and tolerability profiles. Recently, DEX emerged as a Nav1.8 Na+ channel and transient outward K+ (IA) conductance blocker, revealing therefore an unexpected, pleiotypic pharmacodynamic profile. In this study, we performed electrophysiol. experiments in vitro aimed to better characterize the impact of DEX on voltage-dependent currents and synaptic transmission in the hippocampus. By means of patch-clamp recordings on isolated hippocampal neurons, we found that DEX increases outward K+ currents evoked by a voltage ramp protocol. This effect is prevented by the non-selective voltage-dependent K+ channel (Kv) blocker TEA and by the selective small-conductance Ca2+-activated K+ (SK) channel blocker apamin. In keeping with this, extracellular field recordings from rat hippocampal slices also demonstrated that the compound inhibits synaptic transmission and CA1 neuron excitability. Overall, these data further our understanding on the pharmacodynamics of DEX and disclose an addnl. mechanism that could underlie its neuroprotective properties. Also, they identify DEX as a lead to develop new modulators of K+ conductances. The experimental process involved the reaction of 2-Ethylhexyl 2-cyano-3,3-diphenylacrylate(cas: 6197-30-4).Name: 2-Ethylhexyl 2-cyano-3,3-diphenylacrylate

The Article related to dexpramipexole potassium ion cell excitability hippocampus, hippocampal neurons, k+ channels, neuronal excitability, population spike, synaptic transmission, Pharmacology: Effects Of Nervous System- and Behavior-Affecting Drugs and Neuromuscular Agents and other aspects.Name: 2-Ethylhexyl 2-cyano-3,3-diphenylacrylate

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

On May 31, 2007, Ren, Sumei; Mcnamara, Paul; Koharski, David; Hesk, David; Borges, Scott published an article.Computed Properties of 220851-46-7 The title of the article was Synthesis of sulfur-35 reagents for protein labeling. And the article contained the following:

Two 35S reagents were developed to radiolabel proteins. The first reagent, Me35SO2NHCH2C6H4CO2H-p N-hydroxysuccinimide (NHS) ester (SMSB), acylates the ε-amino group of lysine residues in proteins. The second reagent, aldehyde Me35SO2NHCH2C6H4CH2CH2CHO-p (MSAPPA), labels lysine residues via reductive alkylation. Comparing the two methods, the reductive alkylation method labeled proteins over a broader pH range with higher overall radiochem. yield. The biol. activity of the proteins did not change after labeling with these 35S reagents. The experimental process involved the reaction of tert-Butyl 4-((((benzyloxy)carbonyl)amino)methyl)benzoate(cas: 220851-46-7).Computed Properties of 220851-46-7

The Article related to protein labeling sulfur 35 reagent benzoate phenylpropanal preparation, Benzene, Its Derivatives, and Condensed Benzenoid Compounds: Esters, Acyl Peroxides, Acyl Halides and other aspects.Computed Properties of 220851-46-7

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

On September 24, 2014, Manna, Kuntal; Zhang, Teng; Carboni, Michael; Abney, Carter W.; Lin, Wenbin published an article.Product Details of 1312703-30-2 The title of the article was Salicylaldimine-Based Metal-Organic Framework Enabling Highly Active Olefin Hydrogenation with Iron and Cobalt Catalysts. And the article contained the following:

A robust and porous Zr metal-organic framework, sal-MOF, of UiO topol. was synthesized using a salicylaldimine (sal)-derived dicarboxylate bridging ligand. Postsynthetic metalation of sal-MOF with iron(II) or cobalt(II) chloride followed by treatment with NaBEt3H in THF resulted in Fe- and Co-functionalized MOFs (sal-M-MOF, M = Fe, Co) which are highly active solid catalysts for alkene hydrogenation. Impressively, sal-Fe-MOF displayed very high turnover numbers of up to 145000 and was recycled and reused more than 15 times. This work highlights the unique opportunity of developing MOF-based earth-abundant catalysts for sustainable chem. synthesis. The experimental process involved the reaction of Dimethyl 2′-amino-[1,1′:4′,1”-terphenyl]-4,4”-dicarboxylate(cas: 1312703-30-2).Product Details of 1312703-30-2

The Article related to metal organic framework iron cobalt olefin hydrogenation catalyst, Industrial Organic Chemicals, Leather, Fats, and Waxes: Manufacture Of Industrial Organic Chemicals and other aspects.Product Details of 1312703-30-2

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

On March 26, 2020, Follows, Bruce; Kayser-Bricker, Katherine J.; Talbot, Adam Charles; Mente, Scot; Shelekhin, Tatiana; Ericsson, Anna published a patent.Product Details of 227940-70-7 The title of the patent was Preparation of pyrrolo-pyrrolyl alkanones as ubiquitin specific peptidase 9X inhibitors useful for treatment of cancer. And the patent contained the following:

The disclosure provides novel chem. compounds of formula I useful as inhibitors of ubiquitin specific peptidase 9X (USP9X) useful for treatment of diseases and disorders associated with modulation of USP9X such as cancer. Compounds of formula I [wherein X = CR5R6, CR5, NR5, or N; dashed bonds are independently single or double bonds; Y1, Y2, and Y3 independently = N or CRa; Ra independently = H, halo, or CN; Ring A = (un)substituted 5- to 6-membered aryl, (un)substituted 5- to 6-membered heteroaryl, (un)substituted 5- to 7-membered heterocyclyl, etc.; Z1 = O, S, or NR; Z2 = O or NR; W = CH2 and derivative, O, S, etc.; m = 0 or 1; R1 and R2 independently = H, halo, C1-6alkyl, etc.; R3, R4, R5, R6, R7, R8, R9, and R10 independently = H, (un)substituted C1-6alkyl, (un)substituted C3-8cycloalkyl, etc.; each R independently = H, OH, NH2, O(C1-6alkyl), etc.; B = monocyclic or bicyclic 3- to 14-membered ring] or pharmaceutically acceptable salts thereof, are claimed and exemplified. Example compounds (R)-II and (S)-II were prepared from a multistep preparation culminating in chiral separation (preparation given). Exemplified I were evaluated for USP9X inhibitory activity from which both (R)- and (S)-II isomers demonstrated IC50 between ≤ 0.2μM and ≥ 0.05μM. The experimental process involved the reaction of tert-Butyl 7-benzyl-9-oxo-3,7-diazabicyclo[3.3.1]nonane-3-carboxylate(cas: 227940-70-7).Product Details of 227940-70-7

The Article related to pyrrolopyrrolyl alkanone preparation ubiquitin specific peptidase9x inhibitor cancer, Heterocyclic Compounds (More Than One Hetero Atom): Other 5-Membered Rings, Two Or More Hetero Atoms and other aspects.Product Details of 227940-70-7

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

On September 7, 2021, Huang, Huidan; Zhu, Li; Zhang, Chao; Liu, Xiaoping published a patent.COA of Formula: C17H26O7S The title of the patent was Preparation of hydroxypyranone based compound for targeting ubiquitination and degradation of tyrosinase. And the patent contained the following:

The present invention relates to the preparation of hydroxypyranone based compound for targeting ubiquitination and degradation of tyrosinase. In particular the hydroxypyranone based compound I and II (wherein, the linking chain I = triazole derivative or acetamide derivative, the linking chain II = triazole derivative) was prepared According to the inventive method, a Tyr inhibitor, kojic acid, is covalently bound to Pomalidomide or a VHL enzyme targeting ligand via a connecting chain to obtain a compound targeting a Ubiquitinated degradation tyrosinase with a specific structure; the inventive method has simple operation and mild conditions; the inventive product can significantly inhibit the activity of a vegetable, inhibit the production of melanin, have a significant anti-melanoma effect, can significantly prolong the insurance period of a tyrosinase and fruit and have broad application prospects in medicine, food and cosmetics. The experimental process involved the reaction of tert-Butyl 2-(2-(2-(tosyloxy)ethoxy)ethoxy)acetate(cas: 882518-89-0).COA of Formula: C17H26O7S

The Article related to hydroxypyranone derivative preparation tyrosinase inhibitor, Heterocyclic Compounds (More Than One Hetero Atom): Other 5-Membered Rings, Two Or More Hetero Atoms and other aspects.COA of Formula: C17H26O7S

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

On November 6, 2020, Li, Gonglin; Liu, Mohuizi; Zou, Sijia; Feng, Xiaoming; Lin, Lili published an article.Formula: C19H26N2O3 The title of the article was A Bispidine-Based Chiral Amine Catalyst for Asymmetric Mannich Reaction of Ketones with Isatin Ketimines. And the article contained the following:

A unique chiral amine organocatalyst with a bispidine structure was found to be efficient for the diastereo- and enantioselective Mannich reaction of isatin ketimines with ketones. A series of 3-substituted 3-amino-2-oxindoles, e.g., I, bearing vicinal tertiary and quaternary chiral stereogenic centers were obtained in excellent yields with excellent dr and ee values. The gram-scale synthesis and transformation of the product showed the practicability of this methodol. In addition, a possible transition state model was proposed to explain the origin of the stereoselectivity. The experimental process involved the reaction of tert-Butyl 7-benzyl-9-oxo-3,7-diazabicyclo[3.3.1]nonane-3-carboxylate(cas: 227940-70-7).Formula: C19H26N2O3

The Article related to isatin ketimine ketone enantioselective diastereoselective bispidine chiral catalyst mannich, amino oxindole stereoselective preparation, Heterocyclic Compounds (One Hetero Atom): Indoles, Indolizines, Carbazoles, and Other Arenopyrroles and other aspects.Formula: C19H26N2O3

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

On August 13, 2020, Hwang, Jong Yeon; Ha, Jae Du; Cho, Sung Yun; Kim, Pilho; Yun, Chang Soo; Kim, Hyun Jin; Park, Sung Goo; Park, Byoung Chul; Kim, Jeong Hoon; Kim, Sunhong published a patent.SDS of cas: 882518-89-0 The title of the patent was Preparation of target protein EED degradation-inducing degraducer for preventing or treating diseases related to EED, EZH2, or PRC2. And the patent contained the following:

The present invention relates to a target protein degradation-inducing Degraducer, a preparation method thereof, and a pharmaceutical composition for preventing or treating diseases related to EED, EZH2, or PRC2 comprising same as an active ingredient. A novel compound ULB-L-PTM [PTM = EED targeting mols.; L = single bond, chem. linker; ULB = cereblon, MDM2, cIAP, VHL E3 ubiquitin ligase binder] is a Degraducer compound that induces degradation of a target protein, i.e., embryonic ectoderm development (EED) or polycomb repressive complex 2 (PRC2), utilizing cereblon E3 ubiquitin ligase, von Hippel-Lindau tumor suppressor (VHL) E3 ubiquitin ligase, mouse double minute 2 homolog (MDM2) E3 ubiquitin ligase, and cellular inhibitor of apoptosis protein 1 (cIAP) E3 ubiquitin ligase, wherein the compound has an aspect of remarkably achieving target protein degradation-inducing activity through a ubiquitin proteasome system (UPS), and therefore there is a useful effect in that it is possible to provide a pharmaceutical composition for preventing or treating diseases or conditions related to a target protein, and a functional health food composition for preventing or improving same, comprising said compound as an active ingredient. The experimental process involved the reaction of tert-Butyl 2-(2-(2-(tosyloxy)ethoxy)ethoxy)acetate(cas: 882518-89-0).SDS of cas: 882518-89-0

The Article related to preparation target protein eed degradation inducing degraducer, eed ezh2 prc2 disease treatment, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.SDS of cas: 882518-89-0

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

On November 12, 2009, Chesworth, Richard; Shapiro, Gideon; Chantigny, Yves; Mancuso, John; Deziel, Robert published a patent.Safety of tert-Butyl 7-benzyl-9-oxo-3,7-diazabicyclo[3.3.1]nonane-3-carboxylate The title of the patent was Preparation of azabicyclo[2.2.1]heptan-2-yl compounds as HDAC inhibitors and therapeutic uses thereof. And the patent contained the following:

Inhibitors of histone deacetylase of general formula I (wherein R4 is H, C1-C6alkyl, C2-C6 alkenyl, etc.; each A is N, N-oxide, -CH=, and -C(R4)=; Z is -N(R1)OR2 or H; L is a covalent bond or -C0-C3alkyl-N(OR2)-; G2 is C or N; U2 is a covalent bond, -C1-C6alkyl, C3-C6cycloalkyl, etc.; R200, R201, R202 and R203 are independently H, C1-C6alkyl, aryl, etc.; B3 is H, aryl, heteroaryl, etc.; R1 and R2 are independently H, C1-C6alkyl, aryl, etc.) are described together with methods for treating various disorders with such compounds Such disorders include Huntington’s disease, dentatorubralpallidoluysian atrophy, spinal and bulbar muscular atrophy, and spinocerebellar ataxias. Synthetic procedures for preparing I are exemplified, but no biol. data is given. Example compound II was prepared in a 5-step synthesis that involved reaction of intermediate (1S,4S)-2-benzhydryl-2,5-diazabicyclo[2.2.1]heptane 2HCl with Et 2-(methylsulfonyl)pyrimidine-5-carboxylate and reaction of the intermediate formed with hydroxylamine. The experimental process involved the reaction of tert-Butyl 7-benzyl-9-oxo-3,7-diazabicyclo[3.3.1]nonane-3-carboxylate(cas: 227940-70-7).Safety of tert-Butyl 7-benzyl-9-oxo-3,7-diazabicyclo[3.3.1]nonane-3-carboxylate

The Article related to azabicycloheptanyl compound preparation hdac inhibitor nervous system disease treatment, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.Safety of tert-Butyl 7-benzyl-9-oxo-3,7-diazabicyclo[3.3.1]nonane-3-carboxylate

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

On September 30, 2021, Choi, Si Woo; Ryu, Soo Hee; Ryu, Ji Hoon; Son, San Ha; Lee, Hwa Jin; Kim, Seong Hoon; Nam, Boas; Min, Im Suk; Ryu, Hye Guk; Kang, Keum Young published a patent.Reference of tert-Butyl 2-(2-(2-(tosyloxy)ethoxy)ethoxy)acetate The title of the patent was Preparation of pyrimidodiazepine derivatives as PLK1 selective degradation inducers for the treatment and prevention of PLK1-related diseases. And the patent contained the following:

The invention relates to preparation of pyrimidodiazepines that induce selective polo-like kinase 1 (PLK1) degradation Specifically, the invention provides a bifunctional compound in which a PLK1 binding moiety and an E3 ubiquitin ligase-binding moiety are linked by a chem. linker. The example compound I was prepared via 6-steps synthesis using 4-bromobutanoic acid as starting material (procedure given). The compounds of the invention may be effectively utilized in prevention and treatment of PLK1-related diseases. The experimental process involved the reaction of tert-Butyl 2-(2-(2-(tosyloxy)ethoxy)ethoxy)acetate(cas: 882518-89-0).Reference of tert-Butyl 2-(2-(2-(tosyloxy)ethoxy)ethoxy)acetate

The Article related to pyrimidodiazepine preparation plk1 degradation inducer disease treatment prophylaxis, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.Reference of tert-Butyl 2-(2-(2-(tosyloxy)ethoxy)ethoxy)acetate

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