| Autor: |
Mahesh, Radhakrishnan, Dhar, Arghya Kusum, Jindal, Ankur, Bhatt, Shvetank |
| Předmět: |
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| Zdroj: |
Chemical Biology & Drug Design; May2014, Vol. 83 Issue 5, p583-591, 9p |
| Abstrakt: |
A series of novel 1,8-naphthyridine-3-carboxamides as 5- HT3 receptor antagonists were synthesized with an intention to explore the antidepressant activity of these compounds. The title carboxamides were designed using ligand-based approach keeping in consideration the structural requirement of the pharmacophore of 5- HT3 receptor antagonists. The compounds were synthesized using appropriate synthetic route from the starting material nicotinamide. 5- HT3 receptor antagonism of all the compounds, which was denoted in the form of p A2 value, was determined in longitudinal muscle myenteric plexus preparation from guinea-pig ileum against 5- HT3 agonist, 2-methyl-5- HT. Compound 8g (2-methoxy-1, 8-naphthyridin-3-yl) (2-methoxy phenyl piperazine-1-yl) methanone was identified as the most active compound, which expressed a p A2 value of 7.67. The antidepressant activity of all the compounds was examined in mice model of forced swim test ( FST); importantly, none of the compounds was found to cause any significant changes in the locomotor activity of mice at the tested dose levels. In FST, the compounds with considerably higher p A2 value exhibited promising antidepressant-like activity, whereas compounds with lower p A2 value did not show antidepressant-like activity as compared to the control group. [ABSTRACT FROM AUTHOR] |
| Databáze: |
Complementary Index |
| Externí odkaz: |
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