Results 11 to 20 of about 2,057 (83)

The ultra-potent and selective TLR8 agonist VTX-294 activates human newborn and adult leukocytes. [PDF]

PLoS ONE, 2013
Newborns display distinct immune responses that contribute to susceptibility to infection and reduced vaccine responses. Toll-like receptor (TLR) agonists may serve as vaccine adjuvants, when given individually or in combination, but responses of ...
David J Dowling, Zhen Tan, Zofia M Prokopowicz, Christine D Palmer, Maura-Ann H Matthews, Gregory N Dietsch, Robert M Hershberg, Ofer Levy   +7 more
doaj   +1 more source

Iodine(III)‐Mediated Oxidation of Anilines to Construct Dibenzazepines**

Chemistry – A European Journal, Volume 29, Issue 37, July 3, 2023., 2023
Cyclization: A mild, room temperature oxidative cyclization of 2‐substituted anilines that accesses a broad range of medium‐ring N‐heterocycles via radical intermediates is reported. Abstract The development of an efficient process that produces bioactive medium‐sized N‐heterocyclic scaffolds from 2‐substituted anilines using either iodosobenzene or ...
Carmen Margaret White, Naranchimeg Zorigt, Tianning Deng, Tom G. Driver   +3 more
wiley   +1 more source

In Vitro Study of the Metabolic Characteristics of Eight Isoquinoline Alkaloids from Natural Plants in Rat Gut Microbiota

Molecules, 2017
Gut microbiota is populated with an immense number of microorganisms, which can be regulated by dietary components and drugs to markedly affect the nutritional and health status of the host. Eight medicinal isoquinoline alkaloids from natural plants were
Chi-Yu He, Jie Fu, Jia-Wen Shou, Zhen-Xiong Zhao, Long Ren, Yan Wang, Jian-Dong Jiang   +6 more
doaj   +1 more source

Carbotrifluoromethylations of C−C Multiple Bonds (Excluding Aryl‐ and Alkynyltrifluoromethylations)

Chemistry – A European Journal, Volume 29, Issue 19, April 3, 2023., 2023
One main method for the access of organofluorine compounds is the trifluoromethylative functionalization of an olefin bond, which simultaneously introduces a functional group and a trifluoromethyl element into an olefin framework. This review provides a concise overview of this powerful and versatile method. Abstract Organofluorine chemistry has become
Klára Aradi, Loránd Kiss
wiley   +1 more source

Crystal structure of (1S*,2R*)-7-benzyloxy-2-methyl-3-tosyl-2,3,4,5-tetrahydro-1H-3-benzazepin-1-ol: elucidation of the relative configuration of potent allosteric GluN2B selective NMDA receptor antagonists

Acta Crystallographica Section E: Crystallographic Communications, 2016
In the title compound, C25H27NO4S, which crystallized as a racemate, the relative configuration of the adjacent OH and CH3 groups on the azepine ring is trans. The seven-membered azepin ring has a chair-like conformation. The planar aromatic rings of the
Bastian Tewes, Bastian Frehland, Roland Fröhlich, Bernhard Wünsch   +3 more
doaj   +1 more source

Antidiuretic Effects of a Novel Nonpeptide Vasopressin V2-Receptor Agonist, OPC-51803, Administered Orally to Dogs

Journal of Pharmacological Sciences, 2004
We elucidated the pharmacological properties of a novel nonpeptide vasopressin V2-receptor agonist, OPC-51803 ((5R)-2-[1-(2-chloro-4-(1-pyrrolidinyl)benzoyl-2,3,4,5-tetra-hydro-1H-1-benzazepine-5-yl]-N-isopropylacetamide), via both in vitro binding ...
Shigeki Nakamura, Takahiro Hirano, Toshiyuki Onogawa, Shuji Itoh, Ayako Hashimoto, Yoshitaka Yamamura, Kazumi Kondo, Toyoki Mori, Toshimi Kambe   +8 more
doaj   +1 more source

Neurobehavioral phenotyping of Gaq knockout mice reveals impairments in motor functions and spatial working memory without changes in anxiety or behavioral despair

Frontiers in Behavioral Neuroscience, 2012
Many neurotransmitters, hormones and sensory stimuli elicit their cellular responses through the targeted activation of receptors coupled to Gq family heterotrimeric G proteins.
Aliya L Frederick, Aliya L Frederick, Tommy P Saborido, Tommy P Saborido, Gregg D Stanwood, Gregg D Stanwood, Gregg D Stanwood   +6 more
doaj   +1 more source

Evacetrapib is a novel, potent, and selective inhibitor of cholesteryl ester transfer protein that elevates HDL cholesterol without inducing aldosterone or increasing blood pressure

Journal of Lipid Research, 2011
Cholesteryl ester transfer protein (CETP) catalyses the exchange of cholesteryl ester and triglyceride between HDL and apoB containing lipoprotein particles.
Guoqing Cao, Thomas P. Beyer, Youyan Zhang, Robert J. Schmidt, Yan Q. Chen, Sandra L. Cockerham, Karen M. Zimmerman, Sotirios K. Karathanasis, Ellen A. Cannady, Todd Fields, Nathan B. Mantlo   +10 more
doaj   +1 more source

Unravelling benzazepines and aminopyrimidine as multi-target therapeutic repurposing drugs for EGFR V774M mutation in neuroglioma patients [PDF]

BioImpacts
Introduction: Neuroglioma, a classification encompassing tumors arising from glial cells, exhibits variable aggressiveness and depends on tumor grade and stage.
Jitender Singh, Krishan L Khanduja, Pramod K Avti   +2 more
doaj   +1 more source

Fe‐Catalyzed α‐C(sp3)−H Amination of N‐Heterocycles

Angewandte Chemie, Volume 137, Issue 5, January 27, 2025.
An iron(II)‐catalyzed α‐selective C−H amination of N‐heterocycles is reported. It employs the N‐heterocycle as the limiting reagent and presumably involves the formation of a reactive Fe‐nitrene/imidyl radical species. This operationally simple method is amenable to the late‐stage functionalization of natural products and APIs.
Andrea Geraci, Olivier Baudoin
wiley   +2 more sources