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DC Field | Value | Language |
---|---|---|
dc.contributor.author | Mahesh, R. | - |
dc.date.accessioned | 2023-11-20T06:43:09Z | - |
dc.date.available | 2023-11-20T06:43:09Z | - |
dc.date.issued | 2010-11 | - |
dc.identifier.uri | https://www.sciencedirect.com/science/article/abs/pii/S0960894X10012643 | - |
dc.identifier.uri | http://dspace.bits-pilani.ac.in:8080/xmlui/handle/123456789/13175 | - |
dc.description.abstract | A novel series of quinoxalin-2-carboxamides were designed based on the ligand-based approach, employing a three-point pharmacophore model; it consists of an aromatic residue and a linking carbonyl group and a basic nitrogen. The target new chemical entities were synthesized from the key intermediate, quinoxalin-2-carboxylic acid, by coupling it with various amines in the presence of 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride (EDC·HCl) and 1-hydroxybenzotriazole (HOBt). The obtained compounds’ structures were confirmed by spectral data. The target new chemical entities were evaluated for their 5-HT3 receptor antagonisms in longitudinal muscle myenteric plexus preparation from guinea pig ileum against 5-HT3 agonist, 2-methyl-5-HT, which was expressed in the form of pA2 value. All the synthesized compounds showed antagonism towards 5-HT3 receptor; based on this result, a structure–activity relationship was derived, which reveals that the aromatic residue in 5-HT3 receptor antagonists may have hydrophobic interaction with 5-HT3 receptor. Regardless of their antagonistic potentials, all the synthesized molecules were screened for their anti-depressant potentials by using forced swim test in mice model; interestingly none of the tested compounds affect the locomotion of mice in the tested dose levels. Compounds with significant pA2 values exhibited good anti-depressant-like 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 | EDC·HCl | en_US |
dc.subject | Hydroxybenzotriazole (HOBt) | en_US |
dc.subject | Ethylcarbodiimide hydrochloride (EDC·HCl) | en_US |
dc.title | Design, synthesis and structure–activity relationship of novel quinoxalin-2-carboxamides as 5-HT3 receptor antagonists for the management of depression | en_US |
dc.type | Article | en_US |
Appears in Collections: | Department of Pharmacy |
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