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Visible-Light-Mediated Aerobic α-Oxygenation of Tetrahydroisoquinolines and Isoindolines Without External Photocatalysts [PDF]

open access: yesMolecules
A visible-light-mediated strategy for the direct oxygenation of N-substituted tetrahydroisoquinolines and isoindolines to the corresponding benzo-fused lactams under clean conditions without using any external photocatalysts has been developed.
Taiqiang Ye   +6 more
doaj   +2 more sources

Anticonvulsant Potential of 1-Aryl-6,7-dimethoxy-1,2,3,4-tetrahydroisoquinolines: Insights from Strychnine and Nicotine Models in In Vivo and In Silico Studies [PDF]

open access: yesPharmaceuticals
Background: Epilepsy is a chronic, non-communicable brain disorder characterized by recurrent seizures. Some derivatives of 1,2,3,4-tetrahydroisoquinolines have demonstrated anticonvulsant effects.
Azizbek A. Azamatov   +7 more
doaj   +2 more sources

Enantioselective synthesis of chiral 2,3-cis-disubstituted piperidines and C1-substituted tetrahydroisoquinolines by asymmetric Cu-catalyzed cyclizative aminoboration [PDF]

open access: yesNature Communications
Chiral N-heterocycles such as piperidines and tetrahydroisoquinolines are privileged structural motifs in drug discovery and pharmaceutical industry.
Dazhuang Zhang   +3 more
doaj   +2 more sources

Evaluation of the Local Anesthetic Activity, Acute Toxicity, and Structure–Toxicity Relationship in Series of Synthesized 1-Aryltetrahydroisoquinoline Alkaloid Derivatives In Vivo and In Silico [PDF]

open access: yesMolecules, 2023
Isoquinoline alkaloids constitute one of the most common classes of alkaloids that have shown a pronounced role in curing various diseases. Finding ways to reduce the toxicity of these molecules and to increase their therapeutic margin is an urgent ...
Azizbek A. Azamatov   +8 more
doaj   +2 more sources

Formal organocatalytic fluoronitromethane addition to tetrahydroisoquinolines through a CDC process [PDF]

open access: yesFrontiers in Chemistry
Recently, green chemistry has attracted significant attention due to societal challenges regarding waste generation and energy consumption. Consequently, cross-dehydrogenative couplings (CDC) have emerged as a premier strategy for C–C bond formation.
Ramon Rios   +3 more
doaj   +2 more sources

In Vitro Synergistic Activity of Combinations of Tetrahydroisoquinolines and Treatment Antibiotics against Multidrug-Resistant Salmonella [PDF]

open access: yesAdvances in Pharmacological and Pharmaceutical Sciences, 2023
The global burden of Salmonella infections remains high due to the emergence of multidrug resistance to all recommended treatment antibiotics. Tetrahydroisoquinolines (THIQs) have demonstrated promising activity against multidrug-resistant (MDR ...
Rita Ayuk Ndip   +4 more
doaj   +2 more sources

Synthesis of Novel 1-Oxo-2,3,4-trisubstituted Tetrahydroisoquinoline Derivatives, Bearing Other Heterocyclic Moieties and Comparative Preliminary Study of Anti-Coronavirus Activity of Selected Compounds

open access: yesMolecules, 2023
A series of novel 1-oxo-2,3,4-trisubstituted tetrahydroisoquinoline (THIQ) derivatives bearing other heterocyclic moieties in their structure were synthesized based on the reaction between homophthalic anhydride and imines.
Meglena I. Kandinska   +8 more
doaj   +1 more source

3′,4′-Dihydro-2′H-spiro[indoline-3,1′-isoquinolin]-2-ones as potential anti-cancer agents: synthesis and preliminary screening [PDF]

open access: yesRoyal Society Open Science, 2020
Both tetrahydroisoquinolines (THIQs) and oxindoles (OXs) display a broad range of biological activities including anti-cancer activity, and are therefore recognized as two privileged scaffolds in drug discovery. In the present study, 24 3′,4′-dihydro-2′H-
Maloba M. M. Lobe, Simon M. N. Efange
doaj   +1 more source

Electrocatalytic C(sp3)–H/C(sp)–H cross-coupling in continuous flow through TEMPO/copper relay catalysis

open access: yesBeilstein Journal of Organic Chemistry, 2021
Electrocatalytic dehydrogenative C(sp3)–H/C(sp)–H cross-coupling of tetrahydroisoquinolines with terminal alkynes has been achieved in a continuous-flow microreactor through 2,2,6,6-tetramethylpiperidine 1-oxyl (TEMPO)/copper relay catalysis.
Bin Guo, Hai-Chao Xu
doaj   +1 more source

Extending the Scope of the New Variant of the Castagnoli–Cushman Cyclocondensation onto o-Methyl Benzoic Acids Bearing Various Electron-Withdrawing Groups in the α-Position

open access: yesMolecules, 2022
Based on the previously reported involvement of homophthalic acid monoesters in the Castagnoli–Cushman reaction-type cyclocondensation with imines, we tested a number of other o-methyl benzoic acids bearing various electron-withdrawing groups in the α ...
Natalia Guranova   +4 more
doaj   +1 more source

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