4-hydroxy-2-quinolones. 178. irreversible chemical modification of chinoxicaine at the position 4 of the quinolone ring

While continuing our investigation in improving the pharmaceutical activities of the local anesthetic Chinoxicaine we have studied the irreversible replacement of its 4-OH group for bioisosteric fragments. For this purpose the synthesis of a series of 4-R-2-oxo-1,2-dihydroquinoline-3-carboxylic acid...

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Veröffentlicht in:	Chemistry of heterocyclic compounds (New York, N.Y. 1965) N.Y. 1965), 2010-11, Vol.46 (7), p.850-855
Hauptverfasser:	Ukrainets, I. V, Tkach, A. A, Kravtsova, V. V, Mamchur, V. I, Kovalenko, E. Yu
Format:	Artikel
Sprache:	eng
Schlagworte:	4-R-2-oxo-1,2-dihydroquinoline-3-carboxylic acids amidation bioisosteric replacement Chemistry Chemistry and Materials Science local anesthetics Organic acids Organic Chemistry Pharmacy
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Beschreibung
Zusammenfassung:	While continuing our investigation in improving the pharmaceutical activities of the local anesthetic Chinoxicaine we have studied the irreversible replacement of its 4-OH group for bioisosteric fragments. For this purpose the synthesis of a series of 4-R-2-oxo-1,2-dihydroquinoline-3-carboxylic acids 2-(diethylamino)ethylamide hydrochlorides has been carried out. The experimental data of the local anesthetic properties of the compounds obtained are given and discussed.
ISSN:	0009-3122 1573-8353
DOI:	10.1007/s10593-010-0593-z