Synthesis, Characterization and Antidepressant activity of 2-Thioxo-5H-Pyrrolo[3,4-D]Pyrimidin-5-One Derivatives.

Selvinthanuja, C (2012) Synthesis, Characterization and Antidepressant activity of 2-Thioxo-5H-Pyrrolo[3,4-D]Pyrimidin-5-One Derivatives. Masters thesis, College of Pharmacy, Madras Medical College, Chennai.

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Depression is the leading cause of disability1 and affecting about 121 million people world wide. Depression can lead to suicide, a tragic fatality associated with the loss of about 850000 lives every year. According to World Health Organization, by the year 2020, depression is projected to reach 2nd place of the ranking of Disability Adjusted Life Year (DALY) calculated for all ages, both sexes. Today depression is already the 2nd cause of DALYs in the age category 15-44 years for both sexes combined. The compounds (IIa-IIg) were synthesized by multicomponent reaction followed by nucleophillic substitution and cyclocondensation reaction. The synthesized compounds were obtained in good yield. The melting points of the synthesized compounds were determined and have been reported uncorrected. Thin layer chromatography was performed on precoated silicagel G plates using suitable mobile phase. The synthesized compounds were characterized by IR, Mass and NMR spectroscopic techniques. Synthesized compounds were subjected to acute oral toxicity studies. The LD50 values of the synthesized compounds (IIa-IIg) were expected to be less than 2000mg/kg bodyweight. All the synthesized compounds were evaluated for their antidepressant activity by forced swim test in mice. The synthesized compounds IIe and IIg were found to be more active than standard fluoxetine. However, neurobiological and basic research as well as clinical studies have shown that the monoamines have the role in the development of depression syndrome. Antidepressant activity is achieved through various mechanism such as Monoamine oxidase inhibition, Selective serotonin transporter inhibition, inhibition of Selective serotonin reuptake and norepinephrine reuptake, Dopamine transporter inhibition, Corticotropin releasing hormone antagonism.

Item Type: Thesis (Masters)
Uncontrolled Keywords: Synthesis; Characterization; Antidepressant activity; Thioxo; Pyrrolo; Pyrimidin; Derivatives
Subjects: PHARMACY > Pharmaceutical Chemistry
Depositing User: Ravindran C
Date Deposited: 12 Jul 2017 06:31
Last Modified: 12 Oct 2017 03:02

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