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. 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

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Abstract

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.

Item Type: Article
Uncontrolled Keywords: 1,8-Naphthyridine; Serotonin 5-HT3 antagonists
Subjects: R Medicine
Divisions: Faculty of Medicine
Depositing User: Ms azrahani halim
Date Deposited: 22 Jul 2013 02:37
Last Modified: 22 Jul 2013 02:37
URI: http://eprints.um.edu.my/id/eprint/8138

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