Results 41 to 50 of about 1,649 (211)
Close collaboration between an Australian drug checking service and an affiliated university laboratory identifies and characterises the novel synthetic opioid N‐pyrrolidino isotonitazene in an expected oxycodone sample presented by a member of the public.
Blake Curtis +3 more
wiley +1 more source
Graph‐based algorithms that enable efficient computations of all H‐bonds present in structures in entire datasets allow us to dissect H‐bond fingerprints that characterize distinct GPCRs and the structures sampled along their activation. Abstract Changes in structure and dynamics elicited by agonist ligand binding at the extracellular side of G protein
Éva Bertalan +3 more
wiley +1 more source
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
Morfinándiének szintézise és átalakítása biológiailag aktív vegyületekké = Synthesis of morphinandienes and their transformation into biologically active compounds [PDF]
Megvalósítottuk a tebainból kiinduló szintézisét különböző 2-alkiltioapomorfinoknak (kulcsvegyület a 2-metiltioapomorfin és ennek N-propil származéka), valamint S-atommal kapcsolt biszaporfin származékoknak, az előállított származékok farmakológiai ...
Csutorás, Csaba
core
Structure-Based Discovery of New Antagonist and Biased Agonist Chemotypes for the Kappa Opioid Receptor [PDF]
The ongoing epidemics of opioid overdose raises an urgent need for effective antiaddiction therapies and addiction-free painkillers. The κ-opioid receptor (KOR) has emerged as a promising target for both indications, raising demand for new chemotypes of ...
Zheng, Zhong +8 more
core +2 more sources
The opium poppy genome and morphinan production [PDF]
Poppy genome reveals evolution of opiates The opium poppy has been a source of painkillers since Neolithic times. Attendant risks of addiction threaten many today. Guo et al. now deliver a draft of the opium poppy genome, which encompasses 2.72 gigabases assembled into 11 chromosomes and predicts more than
Li Guo +10 more
openaire +3 more sources
Characterization of Opioid Agonist Morphine Derivatives with Emphasis on Medicinal Chemistry
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
Fragmentation pathways of drugs of abuse and their metabolites based on QTOF MS/MS and MSE accurate-mass spectra [PDF]
A study of the fragmentation pathways of several classes of drugs of abuse (cannabinoids, ketamine, amphetamine and amphetamine-type stimulants (ATS), cocaine and opiates) and their related substances has been made.
Bijlsma, Lubertus +3 more
core +2 more sources
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
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

