Diversity-oriented synthesis of 1,3-benzodiazepines [PDF]
© 2017 Elsevier Ltd A concise assembly of the 1,3-benzodiazepine core from A 3 -coupling-derived propargylamines and ortho-bromophenylisocyanates is described.
Li, Binbin+7 more
core +2 more sources
SPION nanoparticles for delivery of dopaminergic isoquinoline and benzazepine derivatives
Superparamagnetic iron nanoparticles (SPIONs) have become one of the most useful colloidal systems in nanomedicine. We report here the preparation of new hybrid core@shell systems based on SPION nanoparticles coated with a SiO2 shell (SPION@SiO2) and functionalized with carboxyl groups (SPION@SiO2-COOH).
Lucena-Serrano, Cristina+9 more
openaire +5 more sources
Fe‐Catalyzed α‐C(sp3)−H Amination of N‐Heterocycles
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
Identifying translational science within the triangle of biomedicine [PDF]
Background: The National Institutes of Health (NIH) Roadmap places special emphasis on “bench-to-bedside” research, or the “translation” of basic science research into practical clinical applications.
Weber, Griffin M
core +2 more sources
Arylbenzazepines Are Potent Modulators for the Delayed Rectifier K+ Channel: A Potential Mechanism for Their Neuroprotective Effects [PDF]
(±) SKF83959, like many other arylbenzazepines, elicits powerful neuroprotection in vitro and in vivo. The neuroprotective action of the compound was found to partially depend on its D1-like dopamine receptor agonistic activity. The precise mechanism for
Bernhard, Eric J.+7 more
core +1 more source
Pharmaceutically relevant (hetero)cyclic compounds and natural products from lignin-derived monomers:Present and perspectives [PDF]
Lignin, the richest source of renewable aromatics on the planet, is an intriguing raw material for the construction of value-added aromatics. In the past decade, much progress has been made regarding the development of efficient lignin depolymerization ...
Afanasenko, Anastasiia, Barta, Katalin
core +1 more source
Design, Synthesis, and Evaluation of Tetrasubstituted Pyridines as Potent 5-HT2C Receptor Agonists. [PDF]
A series of pyrido[3,4-d]azepines that are potent and selective 5-HT2C receptor agonists is disclosed. Compound 7 (PF-04781340) is identified as a suitable lead owing to good 5-HT2C potency, selectivity over 5-HT2B agonism, and in vitro ADME properties ...
Allwood, Daniel M+11 more
core +4 more sources
Asymmetric deprotonation of N‐benzyl urea derivatives of nitrogen heterocycles leads to enantioselective insertion of the benzylic substituent into an aromatic C−N bond. Treatment of the ring‐expanded products induces a stereospecific ring‐contraction that results in an overall asymmetric enantioselective one‐carbon enlargement of the heterocycle ...
Rajendra K. Mallick+2 more
wiley +2 more sources
Synthesis and study of biological activity of tetrahydro-1H-[3]-benzazepines [PDF]
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+4 more
core
Notch Antagonists: Potential Modulators of Cancer and Inflammatory Diseases. [PDF]
Notch is a key player in various developmental processes during the embryonic stage as well as in regulating tissue homeostasis, cell differentiation, and stem cell maintenance in adult life.
Dela Golshayan+6 more
core +1 more source