Pharmacophore based synthesis of 3-chloroquinoxaline-2-carboxamides as serotonin(3) (5-HT3) receptor antagonist
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 ac...
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| Format: | Article |
| Language: | English |
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2004
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| Online Access: | http://eprints.um.edu.my/8137/1/Mahesh-2004-Pharmacophore_Based.pdf |
| _version_ | 1796945698487271424 |
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| author | Mahesh, R. Perumal, R.V. Pandi, P.V. |
| author_facet | Mahesh, R. Perumal, R.V. Pandi, P.V. |
| author_sort | Mahesh, R. |
| collection | UM |
| description | 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. |
| first_indexed | 2024-03-06T05:20:33Z |
| format | Article |
| id | um.eprints-8137 |
| institution | Universiti Malaya |
| language | English |
| last_indexed | 2024-03-06T05:20:33Z |
| publishDate | 2004 |
| record_format | dspace |
| spelling | um.eprints-81372014-10-20T02:41:19Z http://eprints.um.edu.my/8137/ Pharmacophore based synthesis of 3-chloroquinoxaline-2-carboxamides as serotonin(3) (5-HT3) receptor antagonist Mahesh, R. Perumal, R.V. Pandi, P.V. R Medicine 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. 2004 Article PeerReviewed application/pdf en http://eprints.um.edu.my/8137/1/Mahesh-2004-Pharmacophore_Based.pdf 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, |
| spellingShingle | R Medicine Mahesh, R. Perumal, R.V. Pandi, P.V. Pharmacophore based synthesis of 3-chloroquinoxaline-2-carboxamides as serotonin(3) (5-HT3) receptor antagonist |
| title | Pharmacophore based synthesis of 3-chloroquinoxaline-2-carboxamides as serotonin(3) (5-HT3) receptor antagonist |
| title_full | Pharmacophore based synthesis of 3-chloroquinoxaline-2-carboxamides as serotonin(3) (5-HT3) receptor antagonist |
| title_fullStr | Pharmacophore based synthesis of 3-chloroquinoxaline-2-carboxamides as serotonin(3) (5-HT3) receptor antagonist |
| title_full_unstemmed | Pharmacophore based synthesis of 3-chloroquinoxaline-2-carboxamides as serotonin(3) (5-HT3) receptor antagonist |
| title_short | Pharmacophore based synthesis of 3-chloroquinoxaline-2-carboxamides as serotonin(3) (5-HT3) receptor antagonist |
| title_sort | pharmacophore based synthesis of 3 chloroquinoxaline 2 carboxamides as serotonin 3 5 ht3 receptor antagonist |
| topic | R Medicine |
| url | http://eprints.um.edu.my/8137/1/Mahesh-2004-Pharmacophore_Based.pdf |
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