Pyrrolopyrazoles: Synthesis, Evaluation and Pharmacological Screening as Antidepressant Agents

(E-pub Ahead of Print)

Author(s): Samar Said Fatahala*, Shahira Nofal, Eman Mahmoud, Rania Helmy Abd El-hameed.

Journal Name: Medicinal Chemistry

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Background: Pyrroles and fused pyrroles are of great interest as biologically active compounds, among these activities; antidepressant activity is of special concern. Objective: Synthesis of a series of pyrrolopyrazoles and their pyrimidine derivatives and their characterization using spectral data to be monitored for antidepressant activity using behavioral techniques. Method: A control group was administered the vehicle i.p., positive control group received fluoxetine as standard and all other groups were administered the tested compounds. The groups were subjected to tail suspension test (TST) to determine the antidepressant activity compared with fluoxetine as a standard drug. The compounds exhibiting antidepressant activity were then used to analyze changes in serotonin (5HT) level in the brain of albino mice. Results: TST results showed that both pyrazoles and pyrazolopyrimidines derivatives exhibit promising anti-depressant activity. Conclusion: Compounds [pyrazoles & pyrazlopyrimidines] showed promising antidepressant activity possibly mediated by the increased levels of 5HT.

Keywords: Anti-depressant assay, Pyrrolopyrazole, Pyrrole, Pyrazolopyrimidine , Synthesis, SAR, Antidepressant

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(E-pub Ahead of Print)
DOI: 10.2174/1573406414666181108090321
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