van der Waals interactions govern C-β-d-glucopyranosyl triazoles' nM inhibitory potency in human liver glycogen phosphorylase.
Sign Up to like & getrecommendations! Published in 2017 at "Journal of structural biology"
DOI: 10.1016/j.jsb.2017.05.001
Abstract: 3-(C-Glucopyranosyl)-5aryl-1,2,4-triazoles with an aryl moiety larger than phenyl have been shown to have strong inhibitory potency (Ki values in the range of upper nM) for human liver glycogen phosphorylase (hlGP), a pharmacologically relevant target for… read more here.
Keywords: van der; potency; liver glycogen; glycogen phosphorylase ... See more keywords
Curcumin analogues exert potent inhibition on human and rat gonadal 3β-hydroxysteroid dehydrogenases as potential therapeutic agents: structure-activity relationship and in silico docking
Sign Up to like & getrecommendations! Published in 2023 at "Journal of Enzyme Inhibition and Medicinal Chemistry"
DOI: 10.1080/14756366.2023.2205052
Abstract: Abstract Curcuminoids are functional food additives, and the effect on gonadal hormone biosynthesis remains unclear. Gonads contain 3β-hydroxysteroid dehydrogenase isoforms, h3β-HSD2 (humans) and r3β-HSD1 (rats), which catalyse pregnenolone into progesterone. The potency and mechanisms of… read more here.
Keywords: curcumin analogues; inhibition; curcumin; activity ... See more keywords
O-prenylated 3-carboxycoumarins as a novel class of 15-LOX-1 inhibitors
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DOI: 10.1371/journal.pone.0171789
Abstract: Allyloxy, Isopentenyloxy, geranyloxy and farnesyloxy derivatives of 3-carboxycoumarin, at position 5, 6, 7, and 8, were synthesized and their inhibitory potency against human 15-lipoxygenase-1 (human 15-LOX-1) were determined. Among the synthetic coumarins, O-allyl and O-isopentenyl… read more here.
Keywords: lox; class lox; novel class; prenylated carboxycoumarins ... See more keywords
Benzophenone Derivatives with Histamine H3 Receptor Affinity and Cholinesterase Inhibitory Potency as Multitarget-Directed Ligands for Possible Therapy of Alzheimer’s Disease
Sign Up to like & getrecommendations! Published in 2022 at "Molecules"
DOI: 10.3390/molecules28010238
Abstract: The multitarget-directed ligands demonstrating affinity to histamine H3 receptor and additional cholinesterase inhibitory potency represent a promising strategy for research into the effective treatment of Alzheimer’s disease. In this study, a novel series of benzophenone… read more here.
Keywords: cholinesterase inhibitory; inhibitory potency; affinity; directed ligands ... See more keywords