6831-56-7Relevant academic research and scientific papers
Selective inhibition of calcium entry induced by benzylisoquinolines in rat smooth muscle
Anselmi,Fayos,Blasco,Candenas,Cortes,D'Ocon
, p. 337 - 343 (1992)
The mechanism of relaxant activity of six benzylisoquinolines was examined in order to determine the minimal structural requirements that enable these compounds to have either a non-specific action like papaverine or an inhibitory activity on calcium entry via potential-operated channels. All the alkaloids tested totally or partially relaxed KCl-depolarized rat uterus and inhibited oxytocin-induced rhythmic contractions. Only glaucine and laudanosine inhibited K+-induced uterine contractions more than oxytocin-induced uterine contractions. In Ca+-free medium, sustained contractions induced by oxytocin or vanadate were relaxed by the alkaloids tested except for glaucine and laudanosine indicating no inhibitory effect on intracellular calcium release. Those alkaloids containing an unsaturated heterocyclic ring (papaverine, papaverinol, papaveraldine, N-methylpapaverine and dehydropapaverine) exhibited a more specific activity than those with a tetrahydroisoquinoline ring.
Total Synthesis of the Norhasubanan Alkaloid Stephadiamine
Hartrampf, Nina,Winter, Nils,Pupo, Gabriele,Stoltz, Brian M.,Trauner, Dirk
, p. 8675 - 8680 (2018)
(+)-Stephadiamine is an unusual alkaloid isolated from the vine Stephania japonica. It features a norhasubanan skeleton, and contains two adjacent α-tertiary amines, which renders it an attractive synthetic target. Here, we present the first total synthes
COMPOUND LIBRARIES
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Page 79-80, (2010/02/08)
The present invention relates to compounds capable of binding to the active site of protein kinase enzymes. The invention further relates to libraries of compounds and a family of libraries of compounds for use in screening programmes against protein kinases as well as the individual compounds for use in hit to lead and lead optimisation projects, and similar stages in the drug discovery process. The invention also provides methods for making compounds and libraries.
Specific bradycardic agents. 1. Chemistry, pharmacology, and structure-activity relationships of substituted benzazepinones, a new class of compounds exerting antiischemic properties
Reiffen,Eberlein,Muller,Psiorz,Noll,Heider,Lillie,Kobinger,Luger
, p. 1496 - 1504 (2007/10/02)
Structural modification of the calcium-antagonist verapamil (1) by replacement of the lipophilic α-isopropylacetonitrile moiety by various heterocyclic ring systems has led to a new class of cardiovascular compounds which are characterized by a specific bradycardic activity. These agents reduce heart rate without binding to classical calcium channels or β-adrenoceptors, interacting instead specifically with structures at the sino atrial node. Therefore they have also been termed sinus node inhibition. The prototype falipamil (2) has been submitted to furthr optimization mainly hy manipulation of the phthalimidine moiety. This has resultd in a secod generation of specific bradycardic agents with increased potency and selectively and prolonged duration of action represented by the benzazepinone-derivative UL-FS 49 (4). Structure-activity relationships within this novel class of compounds have revealed a marked dependence of activity on the substitution pattern of the aromatic rings, the nature of the central nitrogen atom, and the length of the connecting alkyl chains. The crucial role of the benzazepione ring for bradycardic activity can be best explained by its special impact on the overall molecular conformation.
