Comparative study of dopaminergic activity of tetrahydro-1H-[3]-benzazepines and their precursors [PDF]
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+5 more
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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
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The stabilization of precursors substituted with 2‐, 1‐naphthol via partially aromatic ortho‐quinone methide intermediate was tested with different cyclic imines in [4+2] cycloaddition.8‐Hydroxyquinoline as a formal 1‐naphthol analogue in Mannich reaction was tested.The formed Mannich bases substituted with 2‐ and 1‐naphthol, 5‐chloro‐8 ...
Dóra Hegedűs+3 more
wiley +1 more source
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
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Abstract Background and Purpose Sex‐dependent vascular effects of transient receptor potential (TRP) channels and sex dimorphism in migraine are not yet fully characterized. We investigated the differential vasoactive effects of TRP ankyrin 1 (TRPA1), TRP melastatin 3 (TRPM3) and TRP vanilloid 1 (TRPV1) channels, their pharmacological mechanism(s), and
Eduardo Rivera‐Mancilla+7 more
wiley +1 more source
Study and characterization of modified silicon surfaces with organic molecules [PDF]
Nanostructured thin films and subsequent biofunctionalization of silicon substrates are essential for the development of biosensors devices. The formation of organic monolayers on silicon substrates via Si-C bound allows specific interactions with ...
Contreras-Cáceres, Rafael+5 more
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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
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This review presents an analysis of ten recent total syntheses of cephalotaxine‐type alkaloids published between 2021 and 2024. The structural diversification strategies developed during this period are described. Additionally, a new structural classification system for this alkaloid class is proposed.
Yeju Oh, Anagha Reneesh, Hongjun Jeon
wiley +1 more source
Synthesis of bioactive compounds. Studies of their attachment to nanoparticles [PDF]
The 1-aryl tetrahydroisoquinolines have attracted great attention in medicinal chemistry due to their biological activity. These compounds present antitumor, anti-HIV and antibacterial activities.
Díaz, Amelia+4 more
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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
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