Results 41 to 50 of about 881 (169)
ChemPlusChem, Volume 90, Issue 6, June 2025.Accelerated drug derivatization in microdroplets combined with high‐throughput desorption electrospray ionization mass spectrometry provides rapid reaction screening and label‐free bioassay results, which can expedite drug discovery. Adapting high‐throughput (HT) synthetic methods to the modification of drugs and to testing of their bioactivity should ...
Jyotirmoy Ghosh +3 more
wiley +1 more source
Characterization of Opioid Agonist Morphine Derivatives with Emphasis on Medicinal Chemistry
ChemMedChem, Volume 20, Issue 4, February 16, 2025.The aim of synthesizing new opioid compounds is to produce drugs that are more potent, less addictive, and have fewer side effects, such as respiratory depression and constipation. To achieve this, we evaluated the basicity, lipophilicity, and permeability of 30 opioid compounds, including 11 newly synthesized ones, to better understand the ...
Alaa Malik +7 more
wiley +1 more source
Insights into hydrate formation and stability of morphinanes [PDF]
Acta Crystallographica Section A Foundations and Advances, 2014 The formation of multi-component crystals with water (hydrates) is a widespread phenomenon among organic molecules. Hydrate formation is of high practical relevance for industrially used materials, as it affects their physicochemical properties. [1,2] To exclude water or moisture in industrial processes is often difficult. Therefore knowledge about the
Doris Braun, Ulrich Griesser
openaire +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
Plant Direct, Volume 9, Issue 1, January 2025.ABSTRACT Papaver somniferum L., a medicinal plant renowned for its pharmaceutical alkaloids, has captivated scientific interest due to its rich secondary metabolite profile. This study explores a novel approach to manipulating alkaloid biosynthesis pathways by integrating virus‐induced gene silencing (VIGS) with macerozyme enzyme pretreatment ...
Deniz Ece Özcan +4 more
wiley +1 more source
Development of the Japanese Anticholinergic Risk Scale: English translation of the Japanese article
Geriatrics &Gerontology International, Volume 25, Issue 1, Page 5-13, January 2025.Background Anticholinergic burden, reflecting the cumulative impact of medications with anticholinergic properties, significantly predicts adverse drug reactions and geriatric syndromes in older adults. Although anticholinergic risk scales (ARS) have been developed and validated in various countries, none have been tailored specifically for Japan.
Fumihiro Mizokami +15 more
wiley +1 more source
Scientifica, Volume 2025, Issue 1, 2025.Inflammation helps the immune system identify and eliminate disease‐causing and foreign stimuli and initiate the healing process. Nonsteroidal anti‐inflammatory drugs have been often used in treating inflammation. Synthetic drugs have been associated with severe effects, necessitating the need for alternative medicinal agents.
Stephen Maina Gitahi +4 more
wiley +1 more source
Two‐Step Synthesis of Enantiomerically Pure Morphans from (R)‐Carvone
ChemMedChem, Volume 19, Issue 24, December 16, 2024.A two‐step procedure transformed the natural product (R)‐carvone into enantiomerically pure morphans allowing selective modifications at 2‐, 4‐ and 6/7‐position. Whereas affinity towards opioid receptors could not be detected, nanomolar σ1 affinity was found for indolomorphans and quinolinomorphans.
Giuliana Costanzo +5 more
wiley +1 more source
, 2016 The phenolic group of the potent μ and κ opioid morphinan agonist/antagonists cyclorphan and butorphan was replaced by phenylamino and benzylamino groups including compounds with para-substituents in the benzene ring.
Jean M. Bidlack (1313052) +4 more
core +1 more source
Bivalent and bitopic ligands of the opioid receptors: The prospects of a dual approach
Medicinal Research Reviews, Volume 44, Issue 6, Page 2545-2599, November 2024.Abstract Opioid receptors belonging to the class A G‐protein coupled receptors (GPCRs) are the targets of choice in the treatment of acute and chronic pain. However, their on‐target side effects such as respiratory depression, tolerance and addiction have led to the advent of the ‘opioid crisis’.
Marie Emilie Hovah, Ulrike Holzgrabe
wiley +1 more source