Results 41 to 50 of about 6,452 (247)

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

open access: yes, 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   +5 more
core  

Design, Synthesis, and Evaluation of Tetrasubstituted Pyridines as Potent 5-HT2C Receptor Agonists. [PDF]

open access: yes, 2015
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

Synthesis and Transformations of Bioactive Scaffolds via Modified Mannich and aza‐Friedel–Crafts Reactions

open access: yesThe Chemical Record, EarlyView.
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]

open access: yes, 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   +4 more
core  

Sex differences in the vasoactive effect of transient receptor potential channels: TRPM3 as a new therapeutic target for (neuro)vascular disorders

open access: yesBritish Journal of Pharmacology, Volume 182, Issue 11, Page 2503-2523, June 2025.
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]

open access: yes, 2016
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
core  

Rh(III)‐Catalyzed [5+1] Oxidative Cycloaddition of Arylguanidines with Alkynes: A Novel Access to C4‐Disubstituted 1,4‐ Dihydroquinazolin‐2‐amines [PDF]

open access: yes, 2015
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

Recent Total Syntheses of Cephalotaxine‐Type Alkaloids and Their Structural Diversification (2021–2024): An Update

open access: yesAsian Journal of Organic Chemistry, Volume 14, Issue 3, March 2025.
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]

open access: yes, 2017
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
core  

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]

open access: yes, 2004
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

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