Results 21 to 30 of about 5,203 (175)

The Pictet-Spengler Reaction Updates Its Habits

open access: yesMolecules, 2020
The Pictet-Spengler reaction (P-S) is one of the most direct, efficient, and variable synthetic method for the construction of privileged pharmacophores such as tetrahydro-isoquinolines (THIQs), tetrahydro-β-carbolines (THBCs), and polyheterocyclic ...
Andrea Calcaterra   +9 more
doaj   +1 more source

De Novo Discovery of Nonstandard Thioisoindole‐Bridged Bicyclic Peptides Targeting Traf2‐ and NCK‐Interacting Kinase

open access: yesAngewandte Chemie, EarlyView.
An optimized strategy for the ribosomal synthesis of thioisoindole‐bridged bicyclic (TiB) peptides is incorporated into the RaPID platform, enabling high‐throughput discovery from topologically defined TiB libraries. Proof‐of‐concept selection against TNIK identifies nanomolar‐affinity ligands with inhibitory activity, while x‐ray crystallography ...
Yue Zhang   +5 more
wiley   +2 more sources

Oceanalin B, a Hybrid α,ω-Bifunctionalized Sphingoid Tetrahydroisoquinoline β-Glycoside from the Marine Sponge Oceanapia sp.

open access: yesMarine Drugs, 2021
Oceanalin B (1), an α,ω-bipolar natural product belonging to a rare family of sphingoid tetrahydoisoquinoline β-glycosides, was isolated from the EtOH extract of the lyophilized marine sponge Oceanapia sp.
Tatyana N. Makarieva   +6 more
doaj   +1 more source

Iridium‐Catalyzed Ionic Hydrogenation of Multi‐Aza Heterocycles

open access: yesAngewandte Chemie, EarlyView.
Saturated nitrogen‐containing heterocycles are ubiquitous in bioactive molecules and are thus attractive synthetic targets. A readily accessible cyclometalated iridium(III) complex reduces 14 different aromatic aza heterocycles to (partially)saturated multi aza‐heterocycles enlarging accessible chemical space while displaying high tolerance toward ...
Arthur Despois, Nicolai Cramer
wiley   +2 more sources

Crystal structure and Hirshfeld surface analysis of 2-{[7-acetyl-8-(4-chlorophenyl)-4-cyano-6-hydroxy-1,6-dimethyl-5,6,7,8-tetrahydroisoquinolin-3-yl]sulfanyl}-N-(4-chlorophenyl)acetamide

open access: yesActa Crystallographica Section E: Crystallographic Communications, 2021
In the title molecule, C28H25Cl2N3O3S, the heterocyclic portion of the tetrahydroisoquinoline unit is planar while the cyclohexene ring adopts a twist-boat conformation.
Mehmet Akkurt   +5 more
doaj   +1 more source

Borylcyclopropanes: Synthetic Strategies and Applications

open access: yesAngewandte Chemie, EarlyView.
Borylcyclopropanes (cyclopropanes bearing a boron substituent) sit at the intersection of two privileged frameworks in synthesis. This review provides the first exhaustive survey of their chemistry, spanning metal–carbene, nucleophilic cyclization, radical, hydroboration, and C─H activation routes, and documenting applications in medicinal chemistry ...
Aiza A. Butt, Joseph M. Ready
wiley   +2 more sources

2-[(1R,3S)-6,7-Dimethoxy-1-phenyl-1,2,3,4-tetrahydroisoquinolin-3-yl]-4-phenyl-1,3-thiazole

open access: yesActa Crystallographica Section E, 2011
In the title compound, C26H24N2O2S, the dihedral angle between the thiazole ring and the adjacent phenyl ring is 3.02 (15)°. The N-containing six-membered ring of the tetrahydroisoquinoline unit adopts a half-chair conformation.
Glenn E. M. Maguire   +4 more
doaj   +1 more source

Synthesis and Neurotropic Activity of Novel Quinoline Derivatives

open access: yesMolecules, 1997
Hydroxyalkyl and carboxyalkyl derivatives of silatetrahydroisoquinoline, tetrahydroisoquinoline and tetrahydroquinoline have been synthesized. Their neurotropic activity has been investigated.
Skaidrite Germane   +3 more
doaj   +1 more source

A Class of Promising Acaricidal Tetrahydroisoquinoline Derivatives: Synthesis, Biological Evaluation and Structure-Activity Relationships

open access: yesMolecules, 2014
As part of our continuing research on isoquinoline acaricidal drugs, this paper reports the preparation of a series of the 2-aryl-1-cyano-1,2,3,4-tetrahydroisoquinolines with various substituents on the N-phenyl ring, their in vitro acaricidal activities
Rui Yang   +6 more
doaj   +1 more source

Crystal structure and Hirshfeld surface analysis of 2-{[7-acetyl-4-cyano-6-hydroxy-8-(4-methoxyphenyl)-1,6-dimethyl-5,6,7,8-tetrahydroisoquinolin-3-yl]sulfanyl}acetic acid ethyl ester

open access: yesActa Crystallographica Section E: Crystallographic Communications, 2022
In the title molecule, C25H28N2O5S, (alternative name ethyl 2-{[7-acetyl-4-cyano-6-hydroxy-8-(4-methoxyphenyl)-1,6-dimethyl-5,6,7,8-tetrahydroisoquinolin-3-yl]sulfanyl}acetate) the 4-methoxyphenyl group is disposed on one side of the bicyclic core and ...
Elham A. Al-Taifi   +6 more
doaj   +1 more source

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