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PubMed Journals Articles About "Cyano Fluoro Trifluoromethyl Phenyl Acetamido Phenoxy Benzodthiazol Cyclopropanecarboxamide" RSS

11:22 EDT 20th June 2019 | BioPortfolio

Cyano Fluoro Trifluoromethyl Phenyl Acetamido Phenoxy Benzodthiazol Cyclopropanecarboxamide PubMed articles on BioPortfolio. Our PubMed references draw on over 21 million records from the medical literature. Here you can see the latest Cyano Fluoro Trifluoromethyl Phenyl Acetamido Phenoxy Benzodthiazol Cyclopropanecarboxamide articles that have been published worldwide.

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Showing "Cyano fluoro trifluoromethyl phenyl acetamido phenoxy benzodthiazol cyclopropanecarboxamide" PubMed Articles 1–25 of 604

N-(7-Cyano-6-(4-fluoro-3-(2-(3-(trifluoromethyl)phenyl)acetamido)phenoxy) benzodthiazol-2-yl)cyclopropanecarboxamide (TAK-632) Analogues as Novel Necroptosis Inhibitors by Targeting Receptor-Interacting Protein Kinase 3 (RIPK3): Synthesis, Structure-Activity Relationships and In Vivo Efficacy.

Necroptosis, a form of programmed cell death, plays a critical role in various diseases, including inflammato-ry, infectious and degenerative diseases. We previously identified TAK-632 (6) as a potent inhibitor of necrop-tosis by targeting both RIPK1 and RIPK3 kinases. Herein, we performed three rounds of structural optimizations of TAK-632 and elucidated structure-activity relationships to generate more potent inhibitors by targeting RIPK3. The analogues with carbamide groups exhibited great anti-necroptot...


Visible-Light-Promoted Redox Neutral γ,γ-Difluoroallylation of Cycloketone Oxime Ethers with Trifluoromethyl Alkenes via C-C and C-F Bond Cleavage.

A visible-light-promoted redox neutral γ,γ-difluoroallylation of cycloketone oxime ethers with trifluoromethyl alkenes through C-C and C-F bond cleavage has been achieved, which affords various cyano-substituted gem-difluoroalkenes in generally good yields. The reaction provides a facile protocol for forming gem-difluoroalkene functionality and a cyano group while incorporating them into one molecule. The conversion of the resulting cyano-substituted gem-difluoroalkenes to cyclic monofluoroalkenes via a s...

Efficient green photoluminescence and electroluminescence of iridium complexes with high electron mobility.

Aiming to balance the injection and transport of electrons and holes, nitrogen heterocycle and 1,3,4-oxadiazole derivatives were introduced in iridium(iii) complexes to obtain organic light-emitting diodes (OLEDs) with high performances. Thus, two novel Ir(iii) complexes (Ir(tfmphpm)2(pop) and Ir(tfmppm)2(pop)) with green emissions using 2-(3,5-bis(trifluoromethyl)phenyl)pyrimidine (tfmphpm) and 2-(2,6-bis(trifluoromethyl)pyridin-4-yl)pyrimidine (tfmppm) as cyclometalating ligands, and 2-(5-phenyl-1,3,4-oxa...


EGFR inhibitors from cancer to inflammation: Discovery of 4-fluoro-N-(4-(3-(trifluoromethyl)phenoxy)pyrimidin-5-yl)benzamide as a novel anti-inflammatory EGFR inhibitor.

EGFR inhibitors are well-known as anticancer agents. Quite differently, we report our effort to develop EGFR inhibitors as anti-inflammatory agents. Pyrimidinamide EGFR inhibitors eliciting low micromolar IC and the structurally close non-EGFR inhibitor urea analog were synthesized. Comparing their nitric oxide (NO) production inhibitory activity in peritoneal macrophages and RAW 246.7 macrophages indicated that their anti-inflammatory activity in peritoneal macrophages might be a sequence of EGFR inhibitio...

Forty-Three Fatalities Involving the Synthetic Cannabinoid, 5-Fluoro-ADB: Forensic Pathology and Toxicology Implications.

Forty-three fatalities involving the potent synthetic cannabinoid, 5-Fluoro-ADB, are summarized. For each case, a description of the terminal event, autopsy findings, cause of death, qualitative identification of 5-Fluoro-ADB and its ester hydrolysis metabolite, 5-Fluoro-ADB metabolite 7, in urine, and the quantitative values obtained in the blood specimens are outlined. Central blood concentrations ranged from 0.010 to 2.2 ng/mL for 5-Fluoro-ADB and 2.0 to 166 ng/mL for 5-Fluoro-ADB metabolite 7. Periphe...

Studies towards the development of a PET radiotracer for imaging of the P2Y receptors in the brain: synthesis, F-labeling and preliminary biological evaluation.

Purine nucleotides such as ATP and ADP are important extracellular signaling molecules in almost all tissues activating various subtypes of purinoreceptors. In the brain, the P2Y receptor (P2YR) subtype mediates trophic functions like differentiation and proliferation, and modulates fast synaptic transmission, both suggested to be affected in diseases of the central nervous system. Research on P2YR is limited because suitable brain-penetrating P2YR-selective tracers are not yet available. Here, we describe ...

Functionalized Phenylbenzamides Inhibit Aquaporin-4 Reducing Cerebral Edema and Improving Outcome in Two Models of CNS Injury.

Cerebral edema in ischemic stroke can lead to increased intracranial pressure, reduced cerebral blood flow and neuronal death. Unfortunately, current therapies for cerebral edema are either ineffective or highly invasive. During the development of cytotoxic and subsequent ionic cerebral edema water enters the brain by moving across an intact blood brain barrier and through aquaporin-4 (AQP4) at astrocyte endfeet. Using AQP4-expressing cells, we screened small molecule libraries for inhibitors that reduce AQ...

Organocatalytic Enantioselective Synthesis of α-Fluoro-β-amino Acid Derivatives.

Asymmetric cyclocondensation of N-sulfonylimines with fluoroacetic acid promoted by isothiourea catalyst HBTM-2 generates 3-fluoro-β-lactams with high enantio- and diastereoselectivity. These reactive compounds are opened with alcohols or amines to produce the corresponding α-fluoro-β-amino acid derivatives in moderate yields.

Induction of AMPK activation by N,N'-diarylurea FND-4b decreases growth and increases apoptosis in triple negative and estrogen-receptor positive breast cancers.

Triple negative breast cancer (TNBC) is the most lethal and aggressive subtype of breast cancer. AMP-activated protein kinase (AMPK) is a major energy regulator that suppresses tumor growth, and 1-(3-chloro-4-((trifluoromethyl)thio)phenyl)-3-(4-(trifluoromethoxy)phenyl)urea (FND-4b) is a novel AMPK activator that inhibits growth and induces apoptosis in colon cancer. The purpose of this project was to test the effects of FND-4b on AMPK activation, proliferation, and apoptosis in breast cancer with a particu...

Fungicidal properties of some novel trifluoromethylphenyl amides.

Trifluoromethylphenyl amides (TFMPAs) were designed and synthesized as potential pesticides were designed and synthesized. Thirty three structures were evaluated for fungicidal activity against three Colletotrichum species using direct bioautography assays. Active compounds were subsequently tested against C. fragariae, C. gloeosporioides, C. acutatum, Phomopsis obscurans, P. viticola, Botrytis cinerea and Fusarium oxysporium. The study identified 2-viticolachloro-N-(2,6-dichloro-4-(trifluoromethyl)phenyl)a...

Phenyl Oxidation Impacts the Durability of Alkaline Membrane Water Electrolyzer.

The durability of alkaline anion exchange membrane (AEM) electrolyzers is a critical requirement for implementing this technology in cost-effective hydrogen production. Here, we report that the electrochemical oxidation of the adsorbed phenyl group (found in the ionomer) on oxygen evolution catalysts produces phenol which may cause performance deterioration in AEM electrolyzers. In-line 1H NMR kinetic analyses of phenyl oxidation in a model organic cation electrolyte shows that a catalyst type significantly...

Novel thiosemicarbazones induce high toxicity in estrogen-receptor-positive breast cancer cells (MCF7) and exacerbate cisplatin effectiveness in triple-negative breast (MDA-MB231) and lung adenocarcinoma (A549) cells.

Cis-diamminedichloroplatinum(II) (CDDP), known as cisplatin, has been extensively used against breast cancer, which is the most frequent cancer among women, and lung cancer, the leading cancer that causes death worldwide. Novel compounds such as thiazole derivatives have exhibited antiproliferative activity, suggesting they could be useful against cancer treatment. Herein, we synthesized two novel thiosemicarbazones and an aldehyde to combine with CDDP to enhance efficacy against ER-positive breast MCF7 can...

N-(3-Ethoxy-phenyl)-4-pyrrolidin-1-yl-3-trifluoromethyl-benzamide (EPPTB) prevents 3-iodothyronamine (T1AM)-induced neuroprotection against kainic acid toxicity.

Thyroid hormone and thyroid hormone metabolites, including 3-iodothyronamine (T1AM) and 3-iodothyroacetic acid (TA1), activate AKT signaling in hippocampal neurons affording protection from excitotoxic damage. We aim to explore whether the mechanism of T1AM neuroprotection against kainic acid (KA)-induced excitotoxicity included the activation of the trace amine associated receptor isoform 1 (TAAR1), one of T1AM targets. Rat organotypic hippocampal slices were exposed to vehicle (Veh) or to 5 μM kA for...

Fast beam photofragment translational spectroscopy of the phenoxy radical at 225 nm, 290 nm, and 533 nm.

Photodissociation of the phenoxy radical (C6H5O) is investigated using fast beam photofragment translational spectroscopy. Phenoxy radicals are generated through photodetachment of phenoxide anions (C6H5O-) at 532 nm. Following photoexcitation of the radicals at 225 nm (5.51 eV), 290 nm (4.27 eV), or 533 nm (2.33 eV), photofragments are collected in coincidence to determine their masses, translational energy, and scattering angle for each dissociation event. Two-body dissociation yields exclusively CO + C5H...

Potent 5-Cyano-6-phenyl-pyrimidin-Based Derivatives Targeting DCN1-UBE2M Interaction.

Neddylation of the Cullin-RING E3 ligases (CRLs) regulates the homeostasis of approximately 20% of cellular proteins. Defective in cullin neddylation 1 (DCN1), as a co-E3 ligase, interacts with UBE2M to enhance the activation of CRLs, and this interaction is emerging as a therapeutic target for human diseases. Here, we present a series of pyrimidin-based small molecular inhibitors targeting DCN1-UBE2M interaction. After finding a novel inhibitor DC-1 with IC = 1.2 μM, we performed a series of chemical opti...

Enantioselective Friedel-Crafts Alkylation Reaction of Heteroarenes with N-Unprotected Trifluoromethyl Ketimines by Means of Chiral Phosphoric Acid.

An enantioselective Friedel-Crafts alkylation reaction of pyrroles and indoles with N-unprotected trifluoromethyl ketimines by use of chiral phosphoric acid provided α-trifluoromethylated primary amines bearing chiral quaternary carbon centers in high yields and with high to excellent enantioselectivities. The present reaction is unique to N-unprotected trifluoromethyl ketimines. No reaction took place with N-p-methoxyphenyl (PMP)-substituted ketimine. Corresponding α-trifluoromethylated amines were trans...

Synthesis and urease inhibitory potential of benzophenone sulfonamide hybrid in vitro and in silico.

This study deals with the synthesis of benzophenone sulfonamides hybrids (1-31) and screening against urease enzyme in vitro. Studies showed that several synthetic compounds were found to have good urease enzyme inhibitory activity. Compounds 1 (N'-((4'-hydroxyphenyl)(phenyl)methylene)-4''-nitrobenzenesulfonohydrazide), 2 (N'-((4'-hydroxyphenyl)(phenyl)methylene)-3''-nitrobenzenesulfonohydrazide), 3 (N'-((4'-hydroxyphenyl)(phenyl)methylene)-4''-methoxybenzenesulfonohydrazide), 4 (3'',5''-dichloro-2''-hydrox...

1,2-(Bis)trifluoromethylation of Alkynes: A One-Step Reaction to Install an Underutilized Functional Group.

Modifying the electronic properties of olefins represents the quintessential approach to tuning alkene reactivity. In this context, the exploration of trifluoromethyl groups as divergent electronic modifiers has not been considered. Here, we describe a copper-mediated 1,2-(bis)trifluoromethylation of acetylenes to create-in a single step-E-hexafluorobutenes (E-HFBs). The reaction proceeds with high yield and E/Z selectivity. Since the alkyne captures two trifluoromethyl groups from each molecule of bpyCu(CF...

Photocatalytic, Phosphoranyl Radical-Mediated N-O Cleavage of Strained Cycloketone Oximes.

A photoinduced, phosphoranyl radical-mediated protocol for the direct N-O cleavage of strained cycloketone oximes via a polar/SET crossover process was developed for the first time. This visible-light-driven direct N-O activation mode for oxime offers beneficial features such as streamlined synthetic process and versatile photochemical reactivities. Consequently, the alkenes and α-trifluoromethyl alkenes with varied electronic and structural features acted as competent radical receptors in this protocol, e...

Synthesis of gem-Difluoroalkenes by Merging Ni-Catalyzed C-F and C-C Bond Activation in Cross-Electrophile Coupling.

By merging C-F and C-C bond activation in the cross-electrophile coupling, we developed an efficient cyanide-free synthesis of diverse functional-group-rich cyano-substituted gem-difluoroalkenes using cyclobutanone oxime esters and trifluoromethyl alkenes as precursors. Notably, this Ni-catalyzed reaction is bestowed with broad substrate scope, low catalyst loading, complete regioselectivities, and high tolerance of a wide range of sensitive functional groups. Preliminary mechanistic studies indicate that a...

Hydrogen bonding promoted simple and clean photo-induced reduction of C-X bond with isopropanol.

We herein report a simple and clean photo-induced metal-free reduction of C-X bond under an atmosphere of air at room temperature. Isopropanol is used as both the reducing reagent and solvent. Various functional groups (acids, esters, alcohols, anilines, phenols, indoles, pyridines, cyano and trifluoromethyl groups) and other heterocyclic compounds are tolerated. Different organic halides (including C-I, C-Br and C-Cl bonds) can be dehalogenated with moderate to excellent yields. Polyhalides are also reduce...

A new trifluoromethylated sulfonamide phosphine ligand for Ag(i)-catalyzed enantioselective 3 + 2 cycloaddition of azomethine ylides.

A newly developed Ming-Phos ligand with a 3,5-bis(trifluoromethyl)phenyl substituent was demonstrated to be highly efficient for Ag-catalyzed asymmetric [3 + 2] cycloaddition reactions of azomethine ylides with maleimides, cyclopentene-1,3-diones, and N-(2-t-butylphenyl)maleimide. Being easily prepared on the gram scale in one step, the ligand in combination with a Ag catalyst enables the synthesis of a variety of highly functionalized bicyclic pyrrolidine derivatives in good yields and excellent enantiosel...

Design, synthesis and molecular docking of pyrazolo 3,4d thiazole hybrids as potential anti-HIV-1 NNRT inhibitors.

A series of pyrazolo[3.4,d]thiazole hybrids 6 were synthesized from 5-arylidene-2-imino-3-(4-arylthiazol-2-yl)-thiazolidin-4-ones 5. The 5-arylidene-2-imino-3-(4-arylthiazol-2-yl)-thiazolidin-4-ones 5 were synthesized from 2-amino-4-arylthiazoles 1 and 2-chloro-acetamido-4-arylthiazoles 2 via the formation of 2-imino-3-(4-substituted-arylthiazol-2-yl)-thiazolidin-4-ones 3 using substituted aldehydes 4. The 5-acrylidene derivative 5 on cyclisation with phenyl hydrazine give the pyrazolo [3, 4, d] thiazole de...

Sodium-Catalyzed Friedel-Crafts Reactions and Mechanistic Insight.

Sodium tetrakis[3,5-bis(trifluoromethyl)phenyl]borate (NaBArF) demonstrates catalytic activity for Friedel-Crafts addition reactions of phenolic and other aromatic nucleophiles to trans-β-nitrostyrene. Solubility studies demonstrate a chelating effect between the Na cation and the nitro group of trans-β-nitrostyrene as the basis for catalytic activation. Mechanistic studies are presented, including a comparison with other sodium salts, additive effects, and reaction progress kinetics analysis using F NMR ...

Recent Development of Catalytic Trifluoromethoxylation Reactions.

Trifluoromethoxy (OCF) group exhibits unique properties, which render it a highly desirable structural motif in life and materials sciences. The numbers of newly synthesized trifluoromethyl ethers are booming as new synthetic methods are constantly being developed to access these valuable compounds. This Review summarizes recent catalytic approaches towards preparation of trifluoromethyl ethers. Alkene, allylic, benzylic, and aryl trifluoromethoxylation reactions are discussed herein.


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