Category: 166591-85-1

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Substituted 2-phenylimidazopyridines: A new class of drug leads for human African trypanosomiasis

A phenotypic screen of a compound library for antiparasitic activity on Trypanosoma brucei, the causative agent of human African trypanosomiasis, led to the identification of substituted 2-(3-aminophenyl)oxazolopyridines as a starting point for hit-to-lead medicinal chemistry. A total of 110 analogues were prepared, which led to the identification of 64, a substituted 2-(3-aminophenyl)imidazopyridine. This compound showed antiparasitic activity in vitro with an EC50 of 2 nM and displayed reasonable druglike properties when tested in a number of in vitro assays. The compound was orally bioavailable and displayed good plasma and brain exposure in mice. Compound 64 cured mice infected with Trypanosoma brucei when dosed orally down to 2.5 mg/kg. Given its potent antiparasitic properties and its ease of synthesis, compound 64 represents a new lead for the development of drugs to treat human African trypanosomiasis.

Note that a catalyst decreases the activation energy for both the forward and the reverse reactions and hence accelerates both the forward and the reverse reactions.Formula: C15H19NO4, you can also check out more blogs about166591-85-1

Reference£º
Tetrahydroisoquinoline – Wikipedia,
1,2,3,4-Tetrahydroisoquinoline | C9H11N – PubChem

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Visible light photocatalytic decarboxylative monofluoroalkenylation of alpha-amino acids with: Gem -difluoroalkenes

alpha-Amino acids are among the most common biologically active molecules in nature, and their functionalization has attracted much attention. In this communication, a novel, efficient and general visible-light photocatalytic decarboxylative monofluoroalkenylation of N-protected alpha-amino acids with gem-difluoroalkenes is reported, affording the corresponding alpha-amino monofluoroalkenes which might find applications in medical chemistry and materials science. The reaction proceeded at room temperature with high efficiency and tolerance of various functional groups.

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Reference£º
Tetrahydroisoquinoline – Wikipedia,
1,2,3,4-Tetrahydroisoquinoline | C9H11N – PubChem

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Selective Hydrogenolysis of alpha-C-O Bond in Biomass-Derived 2-Furancarboxylic Acid to 5-Hydroxyvaleric Acid on Supported Pt Catalysts at Near-Ambient Temperature

Hydrogenolysis of the alpha-C-O bond in abundantly available biomass-based furfural and its derivatives provides a viable route for sustainable synthesis of valuable C5 compounds, particularly with two terminal oxygen-containing functional groups. However, efficient cleavage of this bond under mild conditions still remains a crucial challenge, primarily because of the competing cleavage of the alpha-C-O bond and hydrogenation of furan ring. Here, we report that supported Pt catalysts were extremely active for the selective alpha-C-O cleavage in 2-furancarboxylic acid (FCA) hydrogenolysis to synthesize 5-hydroxyvaleric acid (5-HVA), affording a high yield (?78%) on Pt/SiO2 with a Pt particle size of 4.2 nm at an unprecedentedly low temperature of 313 K. In this reaction, the turnover rate and 5-HVA selectivity sensitively depend on the size of the Pt nanoparticles and the underlying support, as a consequence of their effects on the exposed Pt surfaces. Combined reaction kinetic, infrared spectroscopic, and theoretical assessments reveal that while the exposed high-index Pt surfaces (containing higher fraction of step sites) facilitate the kinetically relevant addition of the first H atom to the unsaturated C atom in furan ring and thus the hydrogenolysis activity, the low-index surfaces (containing higher fraction of terrace sites), together with the electron-withdrawing effect of the carboxylic substituent in FCA, favorably stabilize the dangling C2 atom in the transition states of alpha-C-O cleavage and lower their activation barriers, leading to the observed high 5-HVA selectivity. Such pivotal roles of the intrinsic properties of metal surfaces and substituents in tuning the reaction pathways will provide a viable strategy for highly selective upgrading of furan derivatives and other biomass-based oxygenates.

One of the oldest and most widely used commercial enzyme inhibitors is aspirin, Recommanded Product: 2-(tert-Butoxycarbonyl)-1,2,3,4-tetrahydroisoquinoline-1-carboxylic acid, which selectively inhibits one of the enzymes involved in the synthesis of molecules that trigger inflammation. you can also check out more blogs about 166591-85-1

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Tetrahydroisoquinoline – Wikipedia,
1,2,3,4-Tetrahydroisoquinoline | C9H11N – PubChem

Synthetic Route of 166591-85-1, The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.166591-85-1, Name is 2-(tert-Butoxycarbonyl)-1,2,3,4-tetrahydroisoquinoline-1-carboxylic acid, molecular formula is C15H19NO4. In a Patent£¬once mentioned of 166591-85-1

ALPHA SUBSTITUTED CARBOXYLIC ACID AS PPAR MODULATORS

Alpha substituted carboxylic acids of formula (I): wherein R’ and R2 are as defined in the specification and R3 is A) formula (II); B) formula (III); C) formula (IV); and D) formula (V); wherein Y, Art, Are, AP, R4, R5, R6, R7, R6, R9, R9a, R10, R”, R12, R17, ring A, and p are as defined in the specification; pharmaceutical compositions containing effective amounts of said compounds or their salts are useful for treating PPAR, specifically PPAR alpha/y related disorders, such as diabetes, dyslipidemia, obesity and inflammatory disorders. ”

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Tetrahydroisoquinoline – Wikipedia,
1,2,3,4-Tetrahydroisoquinoline | C9H11N – PubChem

Chemistry is traditionally divided into organic and inorganic chemistry. COA of Formula: C15H19NO4, The former is the study of compounds containing at least one carbon-hydrogen bonds.In a patent£¬Which mentioned a new discovery about 166591-85-1

Discovery of 8-Amino-imidazo[1,5-a]pyrazines as Reversible BTK Inhibitors for the Treatment of Rheumatoid Arthritis

Bruton’s tyrosine kinase (BTK) is a Tec family kinase with a well-defined role in the B cell receptor (BCR) pathway. It has become an attractive kinase target for selective B cell inhibition and for the treatment of B cell related diseases. We report a series of compounds based on 8-amino-imidazo[1,5-a]pyrazine that are potent reversible BTK inhibitors with excellent kinase selectivity. Selectivity is achieved through specific interactions of the ligand with the kinase hinge and driven by aminopyridine hydrogen bondings with Ser538 and Asp539, and by hydrophobic interaction of trifluoropyridine in the back pocket. These interactions are evident in the X-ray crystal structure of the lead compounds 1 and 3 in the complex with the BTK enzyme. Our lead compounds show desirable PK profiles and efficacy in the preclinical rat collagen induced arthritis model.

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Reference£º
Tetrahydroisoquinoline – Wikipedia,
1,2,3,4-Tetrahydroisoquinoline | C9H11N – PubChem

Electric Literature of 166591-85-1, The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.166591-85-1, Name is 2-(tert-Butoxycarbonyl)-1,2,3,4-tetrahydroisoquinoline-1-carboxylic acid, molecular formula is C15H19NO4. In a Article£¬once mentioned of 166591-85-1

Green and chemoselective oxidation of alcohols with hydrogen peroxide: A comparative study on Co(II) and Co(III) activity toward oxidation of alcohols

Two new cobalt (II) and cobalt (III) complexes of a terpyridine based ligand, (4?-(2-thienyl)-2,2?;6?,2?-terpyridine (L)), were synthesized. Each complex has two units of the tridentate ligand. The complexes were fully characterized by spectroscopic methods as well as CHN analysis. Moreover, their solid state structures were determined by single crystal X-ray diffraction. The cobaltous complex has the formula [Co(L) 2](NO3)2¡¤2CH3OH¡¤H 2O (1), whereas the cobaltic complex shows the formula [Co(L) 2](NO3)3¡¤2CH3OH (2). Both complexes were tested as homogenous catalysts for the oxidation of a variety of aliphatic and aromatic alcohols utilizing aqueous hydrogen peroxide in water media. The Co(II) complex showed more activity in comparison with its isostructural Co(III) species. The results show that the aromatic alcohols were oxidized with higher conversions and selectivity compared to the aliphatic substrates, possibly due to their conjugation systems which thermodynamically stabilized the carbonyl products.

We¡¯ll also look at important developments in the pharmaceutical industry because understanding organic chemistry is important in understanding health, medicine, the role of 166591-85-1, and how the biochemistry of the body works.Electric Literature of 166591-85-1

Reference£º
Tetrahydroisoquinoline – Wikipedia,
1,2,3,4-Tetrahydroisoquinoline | C9H11N – PubChem

166591-85-1, Name is 2-(tert-Butoxycarbonyl)-1,2,3,4-tetrahydroisoquinoline-1-carboxylic acid, belongs to tetrahydroisoquinoline compound, is a common compound. category: tetrahydroisoquinolineIn an article, once mentioned the new application about 166591-85-1.

Synthesis and biological investigations of 2-(tetrahydropyran-2′-yl) and 2-(tetrahydrofuran-2′-yl)benzimidazoles

A set of benzimidazole derivatives bearing on position 2 a tetrahydropyranyl or tetrahydrofuranyl residue was prepared and tested for antitumoral, anti HIV-1 and other pharmacological activities. While the anti-HIV activity was completely lacking, moderate antitumoral activity was found in a few compounds; particularly the 5,6-dichloro-2-(tetrahydropyran-2-yl)-benzimidazole (8) was able to inhibit the growth of 19 cell lines of humane tumors at near micromolar concentration. On the other hand compounds 4, 6-8 and 10 exhibited significant tracheal relaxant activity in vitro at concentration 3-10 mug/ml, thus resulting superior to theophylline and comparable to amrinone.

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Reference£º
Tetrahydroisoquinoline – Wikipedia,
1,2,3,4-Tetrahydroisoquinoline | C9H11N – PubChem

Synthetic Route of 166591-85-1, Because a catalyst decreases the height of the energy barrier, its presence increases the reaction rates of both the forward and the reverse reactions by the same amount.166591-85-1, Name is 2-(tert-Butoxycarbonyl)-1,2,3,4-tetrahydroisoquinoline-1-carboxylic acid, molecular formula is C15H19NO4. In a article£¬once mentioned of 166591-85-1

Ligand-Accelerated Iron Photocatalysis Enabling Decarboxylative Alkylation of Heteroarenes

A mild, practical protocol for the decarboxylative alkylation of heteroarenes has been accomplished via iron photocatalysis. A diverse range of carboxylic acids readily undergo oxidative decarboxylation and then couple with a broad array of heteroarenes in this transformation. The photoexcited state lifetimes of iron complexes are typically much shorter than those of iridium and ruthenium complexes. Here we describe our effort on iron photocatalysis by utilizing the intramolecular charge transfer pathway of iron-carboxylate complexes.

A reaction mechanism is the microscopic path by which reactants are transformed into products. Each step is an elementary reaction. In my other articles, you can also check out more blogs about 166591-85-1

Reference£º
Tetrahydroisoquinoline – Wikipedia,
1,2,3,4-Tetrahydroisoquinoline | C9H11N – PubChem

Chemistry is an experimental science, and the best way to enjoy it and learn about it is performing experiments. Product Details of 166591-85-1. Introducing a new discovery about 166591-85-1, Name is 2-(tert-Butoxycarbonyl)-1,2,3,4-tetrahydroisoquinoline-1-carboxylic acid

The parmodulin NRD-21 is an allosteric inhibitor of PAR1 Gq signaling with improved anti-inflammatory activity and stability

Novel analogs of the allosteric, biased PAR1 ligand ML161 (parmodulin 2, PM2) were prepared in order to identify potential anti-thrombotic and anti-inflammatory compounds of the parmodulin class with improved properties. Investigations of structure-activity relationships of the western portion of the 1,3-diaminobenzene scaffold were performed using an intracellular calcium mobilization assay with endothelial cells, and several heterocycles were identified that inhibited PAR1 at sub-micromolar concentrations. The oxazole NRD-21 was profiled in additional detail, and it was confirmed to act as a selective, reversible, negative allosteric modulator of PAR1. In addition to inhibiting human platelet aggregation, it showed superior anti-inflammatory activity to ML161 in a qPCR assay measuring the expression of tissue factor in response to the cytokine TNF-alpha in endothelial cells. Additionally, NRD-21 is much more plasma stable than ML161, and is a promising lead compound for the parmodulin class for anti-thrombotic and anti-inflammatory indications.

Note that a catalyst decreases the activation energy for both the forward and the reverse reactions and hence accelerates both the forward and the reverse reactions.Product Details of 166591-85-1, you can also check out more blogs about166591-85-1

Reference£º
Tetrahydroisoquinoline – Wikipedia,
1,2,3,4-Tetrahydroisoquinoline | C9H11N – PubChem

Application of 166591-85-1, The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.166591-85-1, Name is 2-(tert-Butoxycarbonyl)-1,2,3,4-tetrahydroisoquinoline-1-carboxylic acid, molecular formula is C15H19NO4. In a Patent£¬once mentioned of 166591-85-1

AN IMPROVED AND INDUSTRIAL PROCESS FOR THE PREPARATION OF ALFUZOSIN HYDROCHLORIDE AND ITS NOVEL POLYMORPHS

An improved and industrial process for the preparation of Alfuzosin Hydrochloride and its novel polymorphs (Formula (I)).

A reaction mechanism is the microscopic path by which reactants are transformed into products. Each step is an elementary reaction. In my other articles, you can also check out more blogs about 166591-85-1

Reference£º
Tetrahydroisoquinoline – Wikipedia,
1,2,3,4-Tetrahydroisoquinoline | C9H11N – PubChem