Synthesis and antifibrillatory activity of nibentan and its analogues
| Autor: | O. S. Sizova, A. I. L'vov, Sergey D. Yuzhakov, R. G. Glushkov, N. K. Davydova, Svetlana M. Vinogradova, Michail D. Mashkovskiy |
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| Rok vydání: | 2000 |
| Předmět: |
Tertiary amine
medicine.drug_class Stereochemistry Hydrochloride Heart Ventricles Carboxamide Diamines Chemical synthesis Structure-Activity Relationship chemistry.chemical_compound Pentanes Diamine Drug Discovery medicine Animals Ventricular Function Potency Pharmacology Chemistry Organic Chemistry Sematilide General Medicine Electric Stimulation Benzamides Ventricular Fibrillation Cats Anti-Arrhythmia Agents medicine.drug |
| Zdroj: | European Journal of Medicinal Chemistry. 35:205-215 |
| ISSN: | 0223-5234 |
| DOI: | 10.1016/s0223-5234(00)00116-1 |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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