X-ray structures and pharmacological activities of lidocaine derivatives |
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Authors: | Christina Zalaru Mino R Caira Mircea Iovu Elena Cristea |
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Institution: | (1) Department of Organic Chemistry, Faculty of Chemistry, University of Bucharest, 90-92 Panduri Road, Bucharest, Romania;(2) Department of Chemistry, University of Cape Town, Rondebosch, 7701, South Africa;(3) Department of Organic Chemistry, University of Medicine and Pharmaceutics “Carol Davila”, 6 Traian Vuia St., Bucharest, Romania |
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Abstract: | The molecular and crystal structures of the lidocaine analogs 2-(pyrazol-1-yl)-2′-methylacetanilide (1), 2-(3,5-dimethyl-4-iodo-pyrazol-1-yl)-2′-methylacetanilide (2), 2-(3,5-dimethyl-4-iodo-pyrazol-1-yl)-3′-methylacetanilide (3), and 2-(pyrazol-1-yl)-4′-methylacetanilide (4), are reported, with a summary of their pharmacological activities. In this series, the moiety comprising the heterocyclic
ring and the amide alkyl linker displays a common conformation. Molecules of 1–4 form identical hydrogen bonded motifs in their crystals, namely linear chains via intermolecular N–H···O=C hydrogen bonding.
Moderate anesthetic and anti-arrhythmic potencies recorded for 1–4 relative to lidocaine are countered by their significantly lower toxicities. |
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Keywords: | Lidocaine analogs X-ray analysis Hydrogen bonding Anesthetics Anti-arrhythmics |
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