Pharmacophore based synthesis of 3-chloroquinoxaline-2-carboxamides as serotonin(3) (5-HT3) receptor antagonist

Mahesh, R. and Perumal, R.V. and Pandi, P.V. (2004) Pharmacophore based synthesis of 3-chloroquinoxaline-2-carboxamides as serotonin(3) (5-HT3) receptor antagonist. Biological & Pharmaceutical Bulletin, 27 (9). pp. 1403-1405. ISSN 0918-6158

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Abstract

A series of 3-chloroquinoxaline-2-carboxamides were designed and prepared by the condensation of 3-chloro-2-quinoxaloylchloride with appropriate Mannich bases of the p-aminophenol in the microwave environment. The synthesized compounds were evaluated for serotonin(3) (5-HT3) receptor antagonistic activities in longitudinal muscle-myenteric plexus (LMMP) preparation from guinea pig ileum against the 5-HT3 agonist, 2-methyl-5-HT. Compound 3g exhibited comparable 5-HT3 antagonistic activity (pA(2) 6.4) to that of standard antagonist Ondansetron (pA(2) 6.9), while the other compounds exhibited mild to moderate 5-HT3 antagonistic activities.

Item Type: Article
Additional Information: Mahesh, R Perumal, RV Pandi, PV
Uncontrolled Keywords: quinoxalinecarboxamide, Mannich base, serotonin3 (5-HT3) receptor antagonist
Subjects: R Medicine
Divisions: Faculty of Medicine
Depositing User: Ms azrahani halim
Date Deposited: 17 Jul 2013 03:00
Last Modified: 20 Oct 2014 02:41
URI: http://eprints.um.edu.my/id/eprint/8137

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