95092-22-1Relevant academic research and scientific papers
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.
N-(phenylalkylamino-alkyl)-dihydroisoquinolinones, pharmaceutical compositions and methods employing them
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, (2008/06/13)
Compounds of the formula STR1 wherein R1, R2 and R6, which may be identical to or different from each other, are each hydrogen or lower alkyl; R3 is lower alkoxy; R4 is lower alkoxy or, together with R3, methylenedioxy or ethylenedioxy; R5 is hydrogen, lower alkyl or benzyl; R7 is hydrogen or lower alkoxy; R8 is hydrogen, lower alkoxy or, together with R7, methylenedioxy or ethylenedioxy; M is 1 or 2; and N is 2 or 3; And non-toxic, pharmacologically acceptable acid addition salts thereof. The compounds as well as their salts are useful as antihypertensives and heart rate reducers.
