Synthesis and antifibrillatory activity of nibentan and its analogues

Synthesis and antifibrillatory activity of nibentan and its analogues A series of 1,5-diaminopentane derivatives, structurally related to nibentan, was synthesized and tested for antifibrillatory activity. Improved modifications of some known chemical syntheses were proposed. (±)-N-(5-(Diethylamino)-1-(4-nitrophenyl)pentyl)-benzamide hydrochloride, (±)-N-(5-(diethylamino)-1-(4-nitrophenyl)pentyl)-4-nitrobenzamide hydrochloride and (±)-N-(5-(diethylamino)-1-(4-hydroxyphenyl)pentyl)-4-nitrobenzamide hydrochloride were more potent than nibentan and possessed a longer duration of action (up to 5 h in comparison with 60–90 min for nibentan). The antifibrillatory activity of (±)-N-(5-(diethylamino)-1-(4-methoxyphenyl)pentyl)-4-nitrobenzamide hydrochloride was comparable to that of nibentan but exceeded the potency of D-sotalol and sematilide. http://www.deepdyve.com/assets/images/DeepDyve-Logo-lg.png European Journal of Medicinal Chemistry Elsevier

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Publisher
Elsevier
Copyright
Copyright © 2000 Éditions scientifiques et médicales Elsevier SAS
ISSN
0223-5234
eISSN
1768-3254
D.O.I.
10.1016/S0223-5234(00)00116-1
Publisher site
See Article on Publisher Site

Abstract

A series of 1,5-diaminopentane derivatives, structurally related to nibentan, was synthesized and tested for antifibrillatory activity. Improved modifications of some known chemical syntheses were proposed. (±)-N-(5-(Diethylamino)-1-(4-nitrophenyl)pentyl)-benzamide hydrochloride, (±)-N-(5-(diethylamino)-1-(4-nitrophenyl)pentyl)-4-nitrobenzamide hydrochloride and (±)-N-(5-(diethylamino)-1-(4-hydroxyphenyl)pentyl)-4-nitrobenzamide hydrochloride were more potent than nibentan and possessed a longer duration of action (up to 5 h in comparison with 60–90 min for nibentan). The antifibrillatory activity of (±)-N-(5-(diethylamino)-1-(4-methoxyphenyl)pentyl)-4-nitrobenzamide hydrochloride was comparable to that of nibentan but exceeded the potency of D-sotalol and sematilide.

Journal

European Journal of Medicinal ChemistryElsevier

Published: Feb 1, 2000

References

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