Synthesis and Evaluation of New 1,5-Diaryl-3-[4-(methyl-sulfonyl)phenyl]-4,5-dihydro-1H-pyrazole Derivatives as Potential Antidepressant Agents

被引:67
作者
Ozdemir, Ahmet [1 ]
Altintop, Mehlika Dilek [1 ,2 ]
Kaplancikli, Zafer Asim [1 ]
Can, Ozgur Devrim [3 ]
Ozkay, Umide Demir [3 ]
Turan-Zitouni, Gulhan [1 ]
机构
[1] Anadolu Univ, Dept Pharmaceut Chem, Fac Pharm, TR-26470 Eskisehir, Turkey
[2] Anadolu Univ, Grad Sch Hlth Sci, TR-26470 Eskisehir, Turkey
[3] Anadolu Univ, Dept Pharmacol, Fac Pharm, TR-26470 Eskisehir, Turkey
关键词
TAIL SUSPENSION TEST; INVOLVEMENT; DESIGN;
D O I
10.3390/molecules20022668
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
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.
引用
收藏
页码:2668 / 2684
页数:17
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