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Dipeptides which promote release of growth hormone

Compounds of formula (I) are growth hormone releasing peptide mimetics which are useful for the treatment and prevention of osteoporosis. STR1

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

A new application about 6-Methoxy-1,2,3,4-tetrahydroisoquinoline hydrochloride

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Design, synthesis, and biological activity of non-basic compounds as factor Xa inhibitors: SAR study of S1 and aryl binding sites

Compound 7 was identified as the active metabolite of 6 by HPLC and mass spectral analysis. Modification of lead compound 7 by transformation of its N-oxide 6-6 biaryl ring system and fused aromatics produced a series of non-basic fXa inhibitors with excellent potency in anti-fXa and anticoagulant assays. The optimized compounds 73b and 75b showed sub to one digit micromolar anticoagulant activity (PTCT2). Particularly, anti-fXa activity was detected in plasma of rats orally administered with 1 mg/kg of compound 75b.

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

A new application about 6-Methoxy-1,2,3,4-tetrahydroisoquinoline hydrochloride

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Putting the squeeze on CH4 and CO2 through control over interpenetration in diamondoid nets

We report the synthesis, structure, and sorption properties of a family of eight diamondoid (dia) metal-organic materials (MOMs) that are sustained by Co(II) or Zn(II) cations linked by one of three rigid ligands: 4-(2-(4-pyridyl)ethenyl)benzoate (1), 4-(pyridin-4-yl)benzoate (2), and 4-(pyridin-4-yl)acrylate (3). Pore size control in this family of dia nets was exerted by two approaches: changing the length of the linker ligand from 1 to 3, and using solvent as a template to control the level of interpenetration in nets based upon 1 and 3. The resulting MOMs, dia-8i-1, dia-5i-3, dia-7i-1-Zn, dia-7i-1-Co, dia-4i-3-a, dia-4i-3-b, dia-4i-2, and dia-4i-1, exhibit 1D channels with pore limiting diameters (PLDs) of 1.64, 2.90, 5.06, 5.28, 8.57, 8.83, 11.86, and 18.25 A, respectively. We selected dia nets for this study for the following reasons: their 1D channels facilitate study of the impact of pore size on gas sorption parameters in situations where pore chemistry is similar (pyridyl benzoate-type linkers) or identical (in the case of polymorphs), and their saturated metal centers eliminate open metal sites from dominating sorbent-solvate interactions and possibly masking the effect of pore size. Our data reveal that smaller pore sizes offer stronger interactions, as determined by the isosteric heat of adsorption (Qst) and the steepness of the adsorption isotherm in the low-pressure region. The porous MOM with the smallest PLD suitable for physisorption, dia-7i-1-Co, was thereby found to exhibit the highest Qst values for CO2 and CH4. Indeed, dia-7i-1-Co exhibits a Qst for CH4 of 26.7 kJ/mol, which was validated through grand canonical Monte Carlo simulation studies of CH 4 adsorption. This Qst value is considerably higher than those found in covalent organic frameworks and other MOMs with unsaturated metal centers. These results therefore further validate the critical role that PLD plays in gas adsorption by porous MOMs.

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

Awesome Chemistry Experiments For 43207-78-9

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NOVEL TETRAHYDROISOQUINOLINES AND TERAHYDRONAPHTHYRIDINES FOR THE TREATMENT AND PROPHYLAXIS OF HEPATITIS B VIRUS INFECTION

The present invention provides novel compounds having the general formula (I): wherein R1, R 2, R 3, U, V, W, X and Y are as described herein, compositions including the compounds and methods of using the compounds.

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

Extended knowledge of 6,7-Dimethoxy-1,2,3,4-tetrahydroisoquinoline

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Design, synthesis and characterization of novel urolithin derivatives as cholinesterase inhibitor agents

Background: Considering the limitations of current cholinesterase inhibitor drugs for the treatment of Alzheimer?s disease, there is ongoing research activities to find out alternative drug candidates. The aryl-spacer-N-benzyl pharmacophore model has been effectively utilized to design various types of cholinesterase inhibitor molecules, including donepezil. Within this research study, we have questioned the significance of the benzyl group within this pharmacophore employing the urolithin derivatives. Urolithins are benzo[c]chromene analogue metabolites of ellagitannins, abundantly found in pomegranate and berry fruits. Methods: Employing the previous experience that urolithin-spacer-N-benzyl yielded out potent cholinesterase inhibitors, we have designed novel benzo[c]chromene derivatives either lacking the benzyl group or possessing benzyl group in isoquinoline moiety lacking free N-C bond rotation. Following the synthesis and structure identification studies the compounds were screened for their potential to inhibit cholinesterase enzymes. Furthermore, the title compounds were also evaluated for their potential to prevent cholinesterase-accelerated amyloid beta aggregation. In the final, the most active compound was examined to find out its interactions with the cholinesterase enzyme employing a molecular docking study. Results: The title compounds displayed varying cholinesterase inhibitory potential. Some of the compounds were found more / comparable activity to the activity of the current drugs employed in clinic. The potential of the title molecules to inhibit amyloid beta aggregation was found poor. Conclusion: The title compounds displayed varying cholinesterase inhibitory potential, implying that the benzyl group is not a must in each design. This was also shown with the molecular docking studies. On the other hand, the beta amyloid aggregation studies have pointed out that cholinesterase inhibition does not guarantee the prevention of cholinesterase-accelerated amyloid beta aggregation.

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

Final Thoughts on Chemistry for 1745-07-9

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N-substituted isoquinoline derivatives as potential AChE inhibitors

(Chemical Equation Presented) N-substituted donepezil-related isoquinolines have been prepared as potential acetylcholinesterase inhibitors (AChEIs). Microwave assisted procedures and solution-phase parallel synthesis were chosen to optimize the synthetic approach and improve the yields. All synthesized compounds were tested for their AChE inhibitory activity by colorimetric Ellman method and some of them (10, 13, and 28) displayed low inhibitory effects at muM concentrations.

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

Extended knowledge of 6,7-Dimethoxy-1,2,3,4-tetrahydroisoquinoline

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Access to Imidazole Derivatives by Silver(I) Carbonate Mediated Coupling of Vinyl Azides with Secondary Amines

An efficient protocol for the synthesis of structurally diverse imidazoles by Ag2CO3-mediated coupling of vinyl azides with secondary amines was developed, and 22 different examples were synthesized in good to high yields. This operationally simple synthetic strategy allows the formation of three new C-N bonds by cascade reactions that involve sp3 C-H functionalization.

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

Brief introduction of 2-Methyl-1,2,3,4-tetrahydroisoquinoline

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Catalytic asymmetric synthesis of (S)-laudanosine by hydroamination

Lithium amide-chiral bisoxazoline-catalyzed asymmetric intramolecular hydroamination was examined with respect to the structural variants of starting aminoalkenes. Substituents on the nitrogen and olefin of aminoalkenes were found to be important factors affecting reaction efficiency as well as enentioselectivity in the production of chiral tetrahydroisoquinolines and isoindolines. The catalytic asymmetric total synthesis of (S)-laudanosine highlights the utility of the asymmetric hydroamination.

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

Top Picks: new discover of 7-Nitro-1,2,3,4-tetrahydroisoquinoline

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In vitro efficacy of 7-benzylamino-1-isoquinolinamines against Plasmodium falciparum related to the efficacy of chalcones

A series of 1,7-diaminoisoquinolinamines, that are expected to mediate antimalarial activity by the same mechanism employed by the chalcones, were produced. Six 7-benzylamino-1-isoquinolinamines were found to be submicromolar inhibitors in vitro of drug-resistant Plasmodium falciparum, with the best possessing activity comparable to chloroquine. Despite being developed from a lead that is a DHFR inhibitor, these compounds do not mediate their antimalarial effects by inhibition of DHFR.

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

Extracurricular laboratory:new discovery of 7-Chloro-1,2,3,4-tetrahydroisoquinoline

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NOVEL TETRAHYDROISOQUINOLINES AND TERAHYDRONAPHTHYRIDINES FOR THE TREATMENT AND PROPHYLAXIS OF HEPATITIS B VIRUS INFECTION

The present invention provides novel compounds having the general formula (I): wherein R1, R 2, R 3, U, V, W, X and Y are as described herein, compositions including the compounds and methods of using the compounds.

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