dc.contributor.author |
Mahesh, R. |
|
dc.date.accessioned |
2023-11-17T09:55:31Z |
|
dc.date.available |
2023-11-17T09:55:31Z |
|
dc.date.issued |
2011-02 |
|
dc.identifier.uri |
https://www.sciencedirect.com/science/article/abs/pii/S0960894X10018287 |
|
dc.identifier.uri |
http://dspace.bits-pilani.ac.in:8080/xmlui/handle/123456789/13157 |
|
dc.description.abstract |
A novel series of 3-ethoxyquinoxalin-2-carboxamides were designed as per the pharmacophoric requirements of 5-HT3 receptor antagonist using ligand-based approach. The desired carboxamides were synthesized from the key intermediate, 3-ethoxyquinoxalin-2-carboxylic acid by coupling with appropriate amines in the presence of 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride (EDC·HCl) and 1-hydroxybenzotriazole (HOBt). The 5-HT3 receptor antagonism was evaluated in longitudinal muscle myenteric plexus preparation from guinea pig ileum against 5-HT3 agonist, 2-methy-5-HT, which was expressed in the form of pA2 values. Compound 6h (3-ethoxyquinoxalin-2-yl)(4-methylpiperazin-1-yl)methanone was found to be the most active compound, which expressed a pA2 value of 7.7. In forced swim test, the compounds with higher pA2 value exhibited good anti-depressant-like activity and compounds with lower pA2 value failed to show activity as compared to the vehicle-treated group. |
en_US |
dc.language.iso |
en |
en_US |
dc.publisher |
Elsevier |
en_US |
dc.subject |
Pharmacy |
en_US |
dc.subject |
3-ethoxyquinoxalin-2-carboxamides |
en_US |
dc.subject |
Anti-depressants |
en_US |
dc.title |
Discovery of new anti-depressants from structurally novel 5-HT3 receptor antagonists: Design, synthesis and pharmacological evaluation of 3-ethoxyquinoxalin-2-carboxamides |
en_US |
dc.type |
Article |
en_US |