Synthesis and Structure–Active Relationship of 1-Aryl-6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline Anticonvulsants
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概要
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We have previously disclosed that some 6,7-dimethoxyisoquinoline derivatives are able to produce anticonvulsant effects in different animal models of epilepsy. Following these studies this paper describes the synthesis of a small series of new 1-aryl-6,7-dimethoxy-1,2,3,4-tetrahydroisoquinolines strictly related to previously reported analogues. This novel series of isoquinolines was designed on the basis of well defined structure–active relationship (SAR) information already acquired for this class of anticonvulsant agents. The pharmacological effects of the new synthesized compounds were evaluated against audiogenic seizures in Dilute Brown non-Agouti (DBA/2) mice. The preliminary pharmacological screening led to the identification of a new active molecule the 2-acetyl-1-(4′-methylphenyl)-6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline (6d) that displayed significant anticonvulsant activity. Computational studies helped to rationalize these obtained pharmacological results.
著者
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De Luca
Dipartimento Di Matematica E Applicazioni Dell'universita Di Napoli Federico Ii
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De Luca
Dipartimento Di Informatica E Sistemistica Universita Degli Studi Di Roma 'la Sapienza'.
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Gitto Rosaria
Dipartimento Farmaco-Chimico, Università di Messina
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Ferro Stefania
Dipartimento Farmaco-Chimico, Università di Messina
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Agnello Stefano
Dipartimento Farmaco-Chimico, Università di Messina
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Russo Emilio
Dipartimento di Medicina Sperimentale e Clinica, Università Magna Græcia
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De Sarro
Dipartimento di Medicina Sperimentale e Clinica, Università Magna Græcia
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Chimirri Alba
Dipartimento Farmaco-Chimico, Università di Messina
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De Sarro
Dipartimento Di Medicina Sperimentale E Clinica Universita Magna Groecia Di Catanzaro
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Ferro Stefania
Dipartimento Farmaco-Chimico, Università di Messina
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Chimirri Alba
Dipartimento Farmaco-Chimico, Università di Messina
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De Sarro
Dipartimento di Medicina Sperimentale e Clinica, Università Magna Græcia
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Agnello Stefano
Dipartimento Farmaco-Chimico, Università di Messina
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Russo Emilio
Dipartimento di Medicina Sperimentale e Clinica, Università Magna Græcia
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De Luca
Dipartimento Farmaco-Chimico, Università di Messina
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Gitto Rosaria
Dipartimento Farmaco-Chimico, Università di Messina
関連論文
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