90446-70-1Relevant academic research and scientific papers
Aryl substituted aminomethyl benzene derivatives having antiarrhythmic utility
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, (2008/06/13)
The present invention relates to new compounds of the formula STR1 wherein X is STR2 wherein R1 is hydrogen, lower alkyl, phenyl, benzyl, cinnamoyl, thiophene, furan, pyrrole, imidazole, pyrazole oxazole or thiazole; W is hydrogen or hydroxy; (Y)A is positioned ortho to W and is an aminoloweralkyl having the formula --CH2 NR2 R3 where R2 and R3 are the same or different and may be lower alkyl or R2 and R3 may together with N form a pyrrolidine, piperidine or azepine ring, and A is 2; n and m are independently from 0 to 5; and R is straight or branched C1 -C10 alkyl, straight or branched C3 -C10 cycloalkyl, straight or branched C2 -C4 alkenyl or straight or branched C2 -C4 alkynyl, or a pharmaceutically acceptable salt thereof. These compounds are useful in the treatment of various cardiac arrhythmias.
Synthesis and antiarrhythmic and parasympatholytic properties of substituted phenols. 3. Modifications to the linkage region (region 3)
Stout,Matier,Barcelon-Yang,Reynolds,Brown
, p. 295 - 298 (2007/10/02)
As part of a continuing program of systematically modifying the structure of the class I antiarrhythmic drug changrolin, we synthesized 15 analogues in which the linkage between the two aromatic regions was altered. High antiarrhythmic activity and low parasympatholytic activity was found when the linkage region, designated region 3, contained a carbonyl moiety, including ketones, amides, and ureas. Secondary amides were superior to tertiary amides, while amide reversal resulted in no change in activities. One compound in this series, 2,6-bis(1-pyrrolidinyl-methyl)-4-benzamidophenol (ACC-9358), is undergoing preclinical evaluations.
