Results 51 to 60 of about 4,486 (199)

Synthesis and study of biological activity of tetrahydro-1H-[3]-benzazepines [PDF]

, 2017
The 3-Benzazepines are an important class of compounds in drug discovery due to their biological activity such as analgesic, antihypertensive or anticancer properties as well as dopaminergic or antidopaminergic activity. In particular, the tetrahydro-1H-[
Díaz, Amelia, Lucena-Serrano, Ana, Lucena-Serrano, Cristina, López-Romero, Juan Manuel, Valpuesta-Fernandez, Maria   +4 more
core  

Comparative study of dopaminergic activity of tetrahydro-1H-[3]-benzazepines and their precursors [PDF]

, 2016
The discovery of the tetrahydro-1H-[3]-benzazepine SCH23390 [1], represented one of the most important advances in the study of dopaminergic receptors due to their behavior as a selective D1 receptor antagonist.
Contreras-Cáceres, Rafael, Díaz, Amelia, Lucena-Serrano, Cristina, López-Romero, Juan Manuel, Rivera-Ramirez, Alicia, Valpuesta-Fernandez, Maria   +5 more
core  

Cross-dehydrogenative coupling reaction using copper oxide impregnated on magnetite in deep eutectic solvents [PDF]

, 2016
The synthesis of different tetrahydroisoquinolines using choline chloride : ethylene glycol as a deep eutectic solvent (DES) and copper(II) oxide impregnated on magnetite as a catalyst has been accomplished successfully. The copper catalyst amount is the
Marset, Xavier, Pérez Galera, Juana María, Ramón, Diego J.   +2 more
core   +2 more sources

Discovery of Tetrahydroisoquinoline-Based CXCR4 Antagonists [PDF]

ACS Medicinal Chemistry Letters, 2013
A de novo hit-to-lead effort involving the redesign of benzimidazole-containing antagonists of the CXCR4 receptor resulted in the discovery of a novel series of 1,2,3,4-tetrahydroisoquinoline (TIQ) analogues. In general, this series of compounds show good potencies (3-650 nM) in assays involving CXCR4 function, including both inhibition of attachment ...
Valarie M, Truax, Huanyu, Zhao, Brooke M, Katzman, Anthony R, Prosser, Ana A, Alcaraz, Manohar T, Saindane, Randy B, Howard, Deborah, Culver, Richard F, Arrendale, Prahbakar R, Gruddanti, Taylor J, Evers, Michael G, Natchus, James P, Snyder, Dennis C, Liotta, Lawrence J, Wilson   +14 more
openaire   +2 more sources

The One‐Step Synthesis of Biologically Active Isochromans from Lignin‐Derived Aromatic Monomers in Tunable Deep Eutectic Solvents

Chemistry – A European Journal, EarlyView.
A straightforward one‐step protocol enables the synthesis of bio‐based and biologically active isochromans through the Oxa‐Pictet cyclization involving diverse aldehydes, including vanillin in combination with lignin‐derivable homovanillyl alcohol, a prominent aromatic platform chemical obtainable via diol‐assisted fractionation of lignocellulose ...
Anjali Kottayi, Anastasiia M. Afanasenko, Antonio A. Castillo‐Garcia, Walid A. M. Elgaher, Jörg Haupenthal, Anna K. H. Hirsch, Katalin Barta   +6 more
wiley   +1 more source

Toward Rational Understandings of α-C–H Functionalization: Energetic Studies of Representative Tertiary Amines

iScience, 2020
Summary: Functionalization of α-C–H bonds of tertiary amines to build various α-C–X bonds has become a mainstream in synthetic chemistry nowadays. However, due to lack of fundamental knowledge on α-C–H bond strength as an energetic guideline, rational ...
Wenzhi Luo, Jin-Dong Yang, Jin-Pei Cheng
doaj   +1 more source

Stafib‐2‐CR: an Improved Nanomolar and Selective Inhibitor of the Transcription Factor STAT5b Developed by Conformational Restriction of Stafib‐2

Chemistry – A European Journal, EarlyView.
Conformational restriction strategies to increase the activity and selectivity of the STAT5b inhibitor Stafib‐2 are presented. The best conformationally restricted inhibitor Stafib‐2‐CR has threefold higher activity against STAT5b than Stafib‐2. A cell‐permeable prodrug of Stafib‐2‐CR inhibits phosphorylation of STAT5b in cultured human leukemia cells ...
Theresa Münzel, Angela Berg, Christoph Protzel, Sylvie Schäfer, Alexander Jensen‐Feinhals, Thorsten Berg   +5 more
wiley   +1 more source

NADPH oxidase 2 inhibitors CPP11G and CPP11H attenuate endothelial cell inflammation & vessel dysfunction and restore mouse hind-limb flow. [PDF]

, 2019
First described as essential to the phagocytic activity of leukocytes, Nox2-derived ROS have emerged as mediators of a range of cellular and tissue responses across species from salubrious to deleterious consequences.
Camacho, CJ, Cifuentes-Pagano, E, de Jesus, DS, DeVallance, ER, Koes, D, Li, Y, Meijles, DN, Pagano, PJ, Ross, M, Sahoo, S, St Croix, C   +10 more
core   +1 more source

Design, Synthesis, and Photophysical Studies of Functionalized Polyaromatic Isonitriles as Visible Light Photoredox Catalysts

European Journal of Organic Chemistry, EarlyView.
A new series of structurally rich polyaromatic isonitriles is presented as photoredox catalysts. Their photophysical properties are investigated by UV–Vis absorption and fluorescence measurements, combined with experimental and theoretical studies to evaluate both ground‐ and excited‐state redox properties.
Cristina Martini, Camilla Russo, Jussara Amato, Carmine Volpe, Francesca Brunelli, Laurence Grimaud, Maxime R. Vitale, Greta Donati, Andrea Basso, Mariateresa Giustiniano   +9 more
wiley   +1 more source

Covalent drug discovery: Progress against key targets, emerging strategies and lessons learnt

British Journal of Pharmacology, EarlyView.
Abstract Covalent drug discovery is currently experiencing a boom in industrial and academic interest. To date, at least 75 covalent drugs have received regulatory approval, targeting both traditional target classes and more challenging proteins for which other approaches failed. In many cases, unique aspects of covalent targeting are essential for the
Charles P. Brown, Alan Armstrong, David J. Mann   +2 more
wiley   +1 more source