Synthesis of 2-[[1-oxo-2-(substituted amino)propyl]amino]-4,5,6,7-tetrahydrobenzo[b]thiophen-3-carboxylic acid ethyl esters as potential local anesthetic agents

The synthesis of a series of 10 compounds related to 2-[[1-oxo-2-substituted amino)propyl]amino]-4,5,6,7-tetrahydrobenzo[b]thiophen-3-carboxyli c acid ethyl esters (III-XII) that are structurally-related to carticaine and the results of a study of their biological activity are reported. Most of the...

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Bibliographic Details
Published in:	Arzneimittel-Forschung Vol. 45; no. 5; p. 627
Main Author:	al-Obaid, A R
Format:	Journal Article
Language:	English
Published:	Germany 01-05-1995
Subjects:	Anesthetics, Local - chemical synthesis Anesthetics, Local - pharmacology Animals Carticaine - analogs & derivatives Carticaine - chemical synthesis Carticaine - pharmacology Chemical Phenomena Chemistry, Physical Cornea - drug effects Guinea Pigs Lidocaine - pharmacology Magnetic Resonance Spectroscopy Male Pain Measurement - drug effects Rabbits Rana pipiens Reflex - drug effects Skin Tests
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Summary:	The synthesis of a series of 10 compounds related to 2-[[1-oxo-2-substituted amino)propyl]amino]-4,5,6,7-tetrahydrobenzo[b]thiophen-3-carboxyli c acid ethyl esters (III-XII) that are structurally-related to carticaine and the results of a study of their biological activity are reported. Most of the these compounds showed significant activity at lower concentrations when evaluated for local anesthetic activity using the frog-foot withdrawal reflex, the guinea pig wheal derm and the rabbit corneal reflex tests. Compounds III, V, VII and X displayed the shortest onset times and the longest duration of activity, compared to the model drug lidocaine.
ISSN:	0004-4172