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Issue 38, 2016
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Pyridofuropyrrolo[1,2-a]pyrimidines and pyridofuropyrimido[1,2-a]azepines: new chemical entities (NCE) with anticonvulsive and psychotropic properties

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Abstract

Herein we report the synthesis of several new condensed furo[2,3-b]pyridines 3 from the 3-oxo derivatives of cyclopenta[c]pyridine, 5,6,7,8-tetrahydroisoquinoline and pyrano[3,4-c]pyridine 1. The obtained furo[2,3-b]pyridines 3 were used as starting materials for the synthesis of pyridofuropyrrolo[1,2-a]pyrimidines 4 and pyridofuropyrimido[1,2-a]azepines 5. Interestingly enough, derivatives of pyridofuropyrimido[1,2-a]azepines 5 exhibited significantly better anticonvulsant activity than the commercial drug ethosuximide (zarontin). Some of them showed a sedative effect, unlike ethosuximide.

Graphical abstract: Pyridofuropyrrolo[1,2-a]pyrimidines and pyridofuropyrimido[1,2-a]azepines: new chemical entities (NCE) with anticonvulsive and psychotropic properties

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Article information


Submitted
28 Jan 2016
Accepted
06 Mar 2016
First published
31 Mar 2016

RSC Adv., 2016,6, 32234-32244
Article type
Paper

Pyridofuropyrrolo[1,2-a]pyrimidines and pyridofuropyrimido[1,2-a]azepines: new chemical entities (NCE) with anticonvulsive and psychotropic properties

S. N. Sirakanyan, A. Geronikaki, D. Spinelli, R. G. Paronikyan, I. A. Dzhagatspanyan, I. M. Nazaryan, A. H. Akopyan and A. A. Hovakimyan, RSC Adv., 2016, 6, 32234
DOI: 10.1039/C6RA02581A

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