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Microwave assisted synthesis of 2-(4-substituted piperazin-1-yl)-1, 8-naphthyridine-3-carbonitrile as a new class of serotonin 5-HT< sub> 3</sub> receptor antagonists

A series of novel 2-(4-substituted piperazin-1-yl)-1,8-naphthyridine-3-carbonitrile 6 were prepared by microwave irradiation and conventional heating. The intermediate, 2-oxo-1,2-dihydro-1,8-naphthyridine-3-carbonitrile 3, was prepared from 2-aminonicotinaldehyde 1 and ethyl cyanoacetate 2 in the pr...

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Main Authors: Mahesh, R., Venkatesha Perumal, R., Pandi, P.V.
Format: Article
Language:English
Published: 2004
Subjects:
R Medicine
Online Access:http://eprints.um.edu.my/8138/1/Mahesh-2004-Microwave_assisted_s.pdf
http://eprints.um.edu.my/8138/
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spelling my.um.eprints.81382013-07-22T02:37:53Z http://eprints.um.edu.my/8138/ Microwave assisted synthesis of 2-(4-substituted piperazin-1-yl)-1, 8-naphthyridine-3-carbonitrile as a new class of serotonin 5-HT< sub> 3</sub> receptor antagonists Mahesh, R. Venkatesha Perumal, R. Pandi, P.V. R Medicine A series of novel 2-(4-substituted piperazin-1-yl)-1,8-naphthyridine-3-carbonitrile 6 were prepared by microwave irradiation and conventional heating. The intermediate, 2-oxo-1,2-dihydro-1,8-naphthyridine-3-carbonitrile 3, was prepared from 2-aminonicotinaldehyde 1 and ethyl cyanoacetate 2 in the presence of piperidine under solvent free condition. The synthesized compounds were evaluated for 5-HT3 antagonisms in longitudinal muscle-myenteric plexus (LMMP) preparation from Guinea pig ileum against 5-HT3 agonist, 2-methyl-5-HT. Among the compounds tested, 2-(4-allylpiperazin-1-yl)-1,8-naphthyridine-3-carbonitrile 6d showed most favorable 5-HT3 receptor antagonism in the Guinea pig ileum. 2004 Article PeerReviewed application/pdf en http://eprints.um.edu.my/8138/1/Mahesh-2004-Microwave_assisted_s.pdf Mahesh, R. and Venkatesha Perumal, R. and Pandi, P.V. (2004) Microwave assisted synthesis of 2-(4-substituted piperazin-1-yl)-1, 8-naphthyridine-3-carbonitrile as a new class of serotonin 5-HT< sub> 3</sub> receptor antagonists. Bioorganic and Medicinal Chemistry Letters, 14 (20). pp. 5179-5181. ISSN 0960-894X
institution Universiti Malaya
building UM Library
collection Institutional Repository
continent Asia
country Malaysia
content_provider Universiti Malaya
content_source UM Research Repository
url_provider http://eprints.um.edu.my/
language English
topic R Medicine
spellingShingle R Medicine
Mahesh, R.
Venkatesha Perumal, R.
Pandi, P.V.
Microwave assisted synthesis of 2-(4-substituted piperazin-1-yl)-1, 8-naphthyridine-3-carbonitrile as a new class of serotonin 5-HT< sub> 3</sub> receptor antagonists
description A series of novel 2-(4-substituted piperazin-1-yl)-1,8-naphthyridine-3-carbonitrile 6 were prepared by microwave irradiation and conventional heating. The intermediate, 2-oxo-1,2-dihydro-1,8-naphthyridine-3-carbonitrile 3, was prepared from 2-aminonicotinaldehyde 1 and ethyl cyanoacetate 2 in the presence of piperidine under solvent free condition. The synthesized compounds were evaluated for 5-HT3 antagonisms in longitudinal muscle-myenteric plexus (LMMP) preparation from Guinea pig ileum against 5-HT3 agonist, 2-methyl-5-HT. Among the compounds tested, 2-(4-allylpiperazin-1-yl)-1,8-naphthyridine-3-carbonitrile 6d showed most favorable 5-HT3 receptor antagonism in the Guinea pig ileum.
format Article
author Mahesh, R.
Venkatesha Perumal, R.
Pandi, P.V.
author_facet Mahesh, R.
Venkatesha Perumal, R.
Pandi, P.V.
author_sort Mahesh, R.
title Microwave assisted synthesis of 2-(4-substituted piperazin-1-yl)-1, 8-naphthyridine-3-carbonitrile as a new class of serotonin 5-HT< sub> 3</sub> receptor antagonists
title_short Microwave assisted synthesis of 2-(4-substituted piperazin-1-yl)-1, 8-naphthyridine-3-carbonitrile as a new class of serotonin 5-HT< sub> 3</sub> receptor antagonists
title_full Microwave assisted synthesis of 2-(4-substituted piperazin-1-yl)-1, 8-naphthyridine-3-carbonitrile as a new class of serotonin 5-HT< sub> 3</sub> receptor antagonists
title_fullStr Microwave assisted synthesis of 2-(4-substituted piperazin-1-yl)-1, 8-naphthyridine-3-carbonitrile as a new class of serotonin 5-HT< sub> 3</sub> receptor antagonists
title_full_unstemmed Microwave assisted synthesis of 2-(4-substituted piperazin-1-yl)-1, 8-naphthyridine-3-carbonitrile as a new class of serotonin 5-HT< sub> 3</sub> receptor antagonists
title_sort microwave assisted synthesis of 2-(4-substituted piperazin-1-yl)-1, 8-naphthyridine-3-carbonitrile as a new class of serotonin 5-ht< sub> 3</sub> receptor antagonists
publishDate 2004
url http://eprints.um.edu.my/8138/1/Mahesh-2004-Microwave_assisted_s.pdf
http://eprints.um.edu.my/8138/
_version_ 1643688226958868480
score 13.160551

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