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Synthesis and neuroleptic activity of isomeric thieno[1,4]benzothiazines

To investigate the influence of electronic properties of the tricyclic thiazine system on neuroleptic activity, a series of the isomeric N-dimethylaminopropylthienobenzothiazines was synthesized. All compounds were screened for neuroleptic activity in mice and rats. For the active compounds lowest a...

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Published in:	Journal of medicinal chemistry 1975-08, Vol.18 (8), p.857-861
Main Authors:	Grol, C. J, Rollema, H
Format:	Article
Language:	English
Subjects:	Amphetamine - antagonists & inhibitors Animals Humans Male Mice Motor Activity - drug effects Rats Stereotyped Behavior - drug effects Thiazines - chemical synthesis Thiazines - pharmacology Thiophenes - chemical synthesis Thiophenes - pharmacology Tranquilizing Agents - chemical synthesis
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container_issue	8
container_start_page	857
container_title	Journal of medicinal chemistry
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creator	Grol, C. J Rollema, H
description	To investigate the influence of electronic properties of the tricyclic thiazine system on neuroleptic activity, a series of the isomeric N-dimethylaminopropylthienobenzothiazines was synthesized. All compounds were screened for neuroleptic activity in mice and rats. For the active compounds lowest active doses in the antiamphetamine test were determined. Activity appeared to be dependent on the mode of annelation of the thiophene molecule: compunds bearing the same substituent and side chain with the thiophene molecule in 2,3 and 3,4 annelation were active, while those compounds with a 3,2 annelation seemed to be devoid of activity at the given dose.
doi_str_mv	10.1021/jm00242a023
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J ; Rollema, H</creator><creatorcontrib>Grol, C. J ; Rollema, H</creatorcontrib><description>To investigate the influence of electronic properties of the tricyclic thiazine system on neuroleptic activity, a series of the isomeric N-dimethylaminopropylthienobenzothiazines was synthesized. All compounds were screened for neuroleptic activity in mice and rats. For the active compounds lowest active doses in the antiamphetamine test were determined. 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language	eng
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subjects	Amphetamine - antagonists & inhibitors Animals Humans Male Mice Motor Activity - drug effects Rats Stereotyped Behavior - drug effects Thiazines - chemical synthesis Thiazines - pharmacology Thiophenes - chemical synthesis Thiophenes - pharmacology Tranquilizing Agents - chemical synthesis
title	Synthesis and neuroleptic activity of isomeric thieno[1,4]benzothiazines
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