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Issue 54, 2016, Issue in Progress
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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, of 5,6,7,8-tetrahydroisoquinoline and of 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 of pyridofuropyrimido[1,2-a]azepines 5. Interestingly enough, derivatives of pyridofuropyrimido[1,2-a]azepines 5 exhibited anticonvulsant activity significantly better than that of 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
15 Mar 2016
Accepted
11 May 2016
First published
18 May 2016

RSC Adv., 2016,6, 49028-49038
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, 49028
DOI: 10.1039/C6RA06507D

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