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2,3,4,5-Tetrahydro-1H-2-benzazepine (THBA; 1) is nearly 100-fold more selective an inhibitor of phenylethanolamine N-methyltransferase (PNMT, EC 2.1.1.28) versus the alpha2-adrenoceptor than is 1,2,3,4-tetrahydroisoquinoline (THIQ; 2) (1: PNMT Ki = 3.3 muM, alpha2-adrenoceptor Ki = 11 muM, selectivity [alpha2 Ki/PNMT Ki] = 3.3; 2: PNMT Ki = 9.7 muM, alpha2 Ki = 0.35 muM, selectivity = 0.036;). Since the PNMT inhibitory activity and selectivity of THIQ were enhanced by the introduction of a hydrophilic electron-withdrawing 7-substituent and a 3-alkyl-substituent, a similar study was conducted on THBA. 8-Nitro-THBA (3) was found to be as potent an inhibitor of PNMT as its THIQ analogue (21) and to be more selective due to its reduced alpha2-adrenoceptor affinity (3: PNMT Ki = 0.39 muM, alpha2 Ki = 66 muM, selectivity = 170; 21: PNMT Ki = 0.41 muM, alpha2 Ki = 4.3 muM, selectivity = 10). Introduction of a 3-alkyl substituent on the THBA nucleus decreased both the alpha2-adrenoceptor affinity and the PNMT inhibitory activity, suggesting an area of steric bulk intolerance at both sites. 4-Hydroxy-THBA (15), which can be considered a conformationally-restricted analogue of 3-hydroxymethyl-THIQ (30), exhibited poorer PNMT inhibitory activity and less selectivity than 30 (15: PNMT Ki = 58 muM, alpha2 Ki = 100 muM, selectivity = 1.7; 30: PNMT Ki = 1.1 muM, alpha2 Ki = 6.6 muM, selectivity = 6.0). While the addition of an 8-nitro group to 15 increased the selectivity of 16 as compared to its THIQ analogue (31), it was not as potent at PNMT nor as selective as 8-nitro-THBA (3) (16, PNMT Ki = 5.3 muM, alpha2 Ki = 680 muM, selectivity = 130; 31: PNMT Ki = 0.29 muM, alpha2 Ki = 19 muM, selectivity = 66). Compound 3 is the most selective (PNMT/alpha2) and one of the more potent at PNMT compounds yet reported in the benzazepine series, and should have sufficient lipophilicity to penetrate the blood-brain barrier (CLogP = 1.8).

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

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Artificial metalloenzymes, resulting from incorporation of a metal cofactor within a host protein, have received increasing attention in the last decade. The directed evolution is presented of an artificial transfer hydrogenase (ATHase) based on the biotin-streptavidin technology using a straightforward procedure allowing screening in cell-free extracts. Two streptavidin isoforms were yielded with improved catalytic activity and selectivity for the reduction of cyclic imines. The evolved ATHases were stable under biphasic catalytic conditions. The X-ray structure analysis reveals that introducing bulky residues within the active site results in flexibility changes of the cofactor, thus increasing exposure of the metal to the protein surface and leading to a reversal of enantioselectivity. This hypothesis was confirmed by a multiscale approach based mostly on molecular dynamics and protein?ligand dockings.

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The present invention is directed to compounds of the formula I:Wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, X, n and the broken lines are as defined herein which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptor CCR-2.

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

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A concise deracemization of racemic secondary and tertiary amines with a tetrahydroisoquinoline core has been successfully realized by orchestrating a redox process consisted of N-bromosuccinimide oxidation and iridum-catalyzed asymmetric hydrogenation. This compatible redox combination enables one-pot, single-operation deracemization to generate chiral 1-substituted 1,2,3,4-tetrahydroisoquinolines with up to 98% ee in 93% yield, offering a simple and scalable synthetic technique for chiral amines directly from racemic starting materials.

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

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We report herein a protocol for thiolactam preparation with potassium sulfide via visible-light-mediated C(sp3)?H thiocarbonylation, in which polysulfide dianions and radical anions generated from potassium sulfide were the key active species. A variety of thiolactams were straightforward established under mild conditions. Moreover, it was successfully applied to structural modification of tetrahydroberberine.

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Photolysis of O-acyl-N-hydroxy-2-thiopyridone, derived from 2-tetrahydrofuryl carboxylic acid or 2,5 -anhydro -D -allonic acid, gave the corresponding C-nucleoside derivatives in the presence of heteroaromatic compounds via radical pathways.

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

Discover the magic of the 7-Bromo-1,2,3,4-tetrahydroisoquinoline

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The invention belongs to the field of medical technology, in particular to general formula (I) as shown in of tetracyclic Anaplastic lymphoma kinase inhibitor, its pharmaceutically acceptable salt or a stereoisomer thereof, wherein R 1, R 2, R 3, R 4, R 5 and A link like defined in the specification. The invention also relates to methods of preparing such compounds, pharmaceutical preparations comprising these compounds and pharmaceutical composition, the compound and, its pharmaceutically acceptable salts or stereoisomers thereof, in the preparation of the treatment and/or prevention of Anaplastic lymphoma kinase-mediated cancer diseases related to the application of the medicament. (by machine translation)

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New Advances in Chemical Research, May 2021. The appropriate choice of redox mediator can avoid electrode passivation and overpotential, which strongly inhibit the efficient activation of substrates in electrolysis. SDS of cas: 226942-29-6, At least one of the reactants interacts with the solid surface in a physical process called adsorption in such a way. 226942-29-6, name is 6-Bromo-1,2,3,4-tetrahydroisoquinoline. In an article,Which mentioned a new discovery about 226942-29-6

The present invention relates to novel compounds of formula (I) having S1P1 agonist activity, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of various disorders.

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

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A series of alkyloxyquinoline derivatives has been developed to evaluate the relationship between P-gp potency and lipophilicity. The results show a satisfactory lipophilicity-activity correlation although a series of derivatives showing higher P-gp potency is needed in order to confirm this hypothesis.

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

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Amines such as 1,2,3,4-tetrahydroisoquinoline undergo redox-neutral annulations with 2-methyl-3,5-dinitrobenzaldehyde and closely related substrates. Acetic acid serves as the solvent and sole promoter of these transformations which involve dual C-H functionalization.

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