Results 41 to 50 of about 3,116 (182)
Q/R site interactions with the M3 helix in GluK2 kainate receptor channels revealed by thermodynamic mutant cycles [PDF]
, 2013 RNA editing at the Q/R site near the apex of the pore loop of AMPA and kainate receptors controls a diverse array of channel properties, including ion selectivity and unitary conductance and susceptibility to inhibition by polyamines and cis-unsaturated ...
Boland +67 more
core +2 more sources
The Chemical Record, Volume 25, Issue 8, August 2025.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
Pharmaceutically relevant (hetero)cyclic compounds and natural products from lignin-derived monomers:Present and perspectives [PDF]
, 2021 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
British 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
Rigidity versus flexibility: is this an issue in S1 (sigma-1) receptor ligand affinity and activity? [PDF]
, 2016 A set of stereoisomeric 2,5-diazabicyclo[2.2.2]octanes 14 and 15 was prepared in a chiral-pool synthesis starting from (S)- or (R)-aspartate. The key step in the synthesis was a Dieckmann-analogous cyclization of (dioxopiperazinyl)acetates 8, which ...
B\uf6rgel, Frederik +10 more
core +1 more source
Asian 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
Catalytic Cyclization of o‐Alkynyl Phenethylamines via Osmacyclopropene Intermediates: Direct Access to Dopaminergic 3‐Benzazepines [PDF]
, 2015 NOTICE: This is the peer reviewed version of the following article: Álvarez-Pérez, A., González-Rodríguez, C., García-Yebra, C., Varela, J. A., Oñate, E., Esteruelas, M. A., Saá, C. (2015).
Esteruelas Rodrigo, Miguel Ángel +6 more
core +1 more source
One-Pot Phosphate-Mediated Synthesis of Novel 1,3,5-Trisubstituted Pyridinium Salts: A New Family of S. aureus Inhibitors [PDF]
, 2017 Polysubstituted pyridinium salts are valuable pharmacophores found in many biologically active molecules. Their synthesis typically involves the use of multistep procedures or harsh reaction conditions.
Edwards, M +4 more
core +1 more source
Phenol (bio)isosteres in drug design and development
Archiv der Pharmazie, Volume 358, Issue 1, January 2025.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
Microbial Biotechnology, Volume 17, Issue 11, November 2024.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