Abstract
In an effort to develop potent antidepressant agents, new pyrazoline derivatives 2a–s were synthesized and evaluated for their antidepressant-like activity by tail suspension test (TST) and modified forced swimming test (MFST). The effects of the compounds on spontaneous locomotor activity were also investigated using an activity cage apparatus. Among these derivatives, compounds 2b, 2d, 2f, 2o, and 2r decreased both horizontal and vertical activity number of the mice. On the other hand, compounds 2a, 2h, 2j, 2k, 2l, 2m, and 2n, which did not induce any significant change in the locomotor activity, significantly shortened the immobility time of mice in TST and MFST, representing the presence of the antidepressant-like effect. Additionally, the same compounds increased the swimming time of mice in MFST without any change in climbing duration, similar to the reference drug fluoxetine (10 mg/kg). In the light of previous papers examining the effects of pyrazolines on central nervous system, this study, once more, pointed out remarkable antidepressant activity potential of pyrazoline derivatives.
Highlights
Major depressive disorder (MDD) is a multifactorial mood disorder affecting millions of people around the world
Encouraged by the large number of papers regarding the antidepressant potential of pyrazoline scaffold [7,8,9,10,11,12,13,14,15,16,17], we describe the synthesis and in vivo evaluation of some new methylsulfonyl-substituted pyrazoline derivatives as potential antidepressant agents
The synthesis of compounds 2a–s followed the general pathway outlined in Scheme 1
Summary
Major depressive disorder (MDD) is a multifactorial mood disorder affecting millions of people around the world. According to the World Health Organization (WHO), depression is the second leading cause of disability (years of healthy life lost) in patients aged 15–44 years. For 2020, the WHO estimates that depression will become the second leading cause of disability for all age groups. The limited mechanistic understanding of depression pathogenesis and decreased antidepressant treatment response have resulted in the high rate of treatment failures. Hydrazine-based drugs still remain in clinical use for the treatment of depression. Due to their side effects, medicinal chemists have focused on the discovery of new antidepressant agents with enhanced pharmacological activity and limited toxicity via the structural modification of the hydrazine group [7]. Encouraged by the large number of papers regarding the antidepressant potential of pyrazoline scaffold [7,8,9,10,11,12,13,14,15,16,17], we describe the synthesis and in vivo evaluation of some new methylsulfonyl-substituted pyrazoline derivatives as potential antidepressant agents
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