Rh(III)‐Catalyzed [5+1] Oxidative Cycloaddition of Arylguanidines with Alkynes: A Novel Access to C4‐Disubstituted 1,4‐ Dihydroquinazolin‐2‐amines [PDF]
NOTICE: This is the peer reviewed version of the following article: Cajaraville, A., Suárez, J., López, S., Varela. J. A., Saá, C. (2015). Rh(III)‐Catalyzed [5+1] Oxidative Cycloaddition of Arylguanidines with Alkynes: A Novel Access to C4‐Disubstituted ...
Cajaraville Leiro, Ana+4 more
core +1 more source
Synthesis of Benzazepine Alkaloids and Related Compounds
Tetsuji Kametani, Keiichiro Fukumoto
openalex +3 more sources
In vitro activity against Leishmania and human skin permeation of miltefosine ultradeformable liposomes [PDF]
Introducción: los liposomas ultradeformables de miltefosina (LUD-MIL) constituyen una opción para el tratamiento tópico en leishmaniasis cutánea penetrando los estratos de la piel hasta la dermis, sitio donde habita el parásito.
Escobar Rivero, Patricia+2 more
core +1 more source
Conjugation of Organoruthenium(II) 3-(1H-Benzimidazol-2-yl)pyrazolo[3,4-b]pyridines and Indolo[3,2-d]benzazepines to Recombinant Human Serum Albumin: a Strategy To Enhance Cytotoxicity in Cancer Cells [PDF]
Five organoruthenium complexes [RuCl(η6-arene)(L)]Cl with a modified arene ligand, namely, 4-formylphenoxyacetyl-η6-benzylamide, and L = 3-(1H-benzimidazol-2-yl)-1H-pyrazolo[3,4-b]pyridines or indolo[3,2-d]benzazepines were synthesized and conjugated to ...
Ang W. H.+43 more
core +2 more sources
A novel, tandem construction of C-N and C-C bonds: facile and one-pot transformation of the Baylis-Hillman adducts into 2-benzazepines [PDF]
A novel reaction involving tandem construction of C-N and C- C bonds via the simultaneous Ritter and Houben-Hoesch reactions on Baylis-Hillman adducts leading to a convenient, one-pot synthesis of 2-benzazepine derivatives is described.
Basavaiah, Deevi+1 more
core +1 more source
Phenol (bio)isosteres in drug design and development
This review explores the pivotal role of phenol bioisosteres in drug design, highlighting their potential to overcome the limitations of phenolic compounds, such as poor bioavailability and rapid metabolism. By examining diverse bioisosteric replacements, from benzimidazolones to quinolinones, it is demonstrated how these modifications enhance drug ...
Calvin Dunker+2 more
wiley +1 more source
Optimized psilocybin production in tryptophan catabolism‐repressed fungi
Here, we developed an in vivo psilocybin production chassis, based on repression of l‐tryptophan catabolism. By genome mining, we identified two aminotransferase ARO8/9 orthologs in Aspergillus nidulans involved in l‐tryptophan catabolism. Double deletion of the aminotransferase genes aroH1 and aroH2 resulted in a 10‐fold increased psilocybin ...
Slavica Janevska+12 more
wiley +1 more source
Neuroblastoma and its Target Therapies: A Medicinal Chemistry Review
Searching for a cure for neuroblastoma: This review highlights the urgent need to find a cure for high‐risk neuroblastoma. It provides an overview of the current treatment available and the drug discovery approach of seven drugs that reached clinical trial.
A. Gerges, U. Canning
wiley +1 more source
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
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