التفاصيل البيبلوغرافية
| العنوان: |
Design and synthesis of novel PDE4 inhibitors as potential candidates for antidepressant agents. |
| المؤلفون: |
Yingcong Yu, Yan Zhao, Yajing Wang, Xianfeng Huang |
| المصدر: |
Journal of Chemical Research; Sep/Oct2023, Vol. 47 Issue 5, p1-10, 10p |
| مصطلحات موضوعية: |
PHOSPHODIESTERASE inhibitors, ANTIDEPRESSANTS, WATER consumption, CHEMICAL synthesis, IN vitro studies, KETAMINE, IN vivo studies |
| مستخلص: |
PDE4 inhibitors exhibit anti-stress and antidepressant-like abilities by catalyzing the hydrolysis of cAMP, a primary regulator for intracellular communication in the brain. Herein, novel diarylpyrazole derivatives are synthesized and investigated for their ability to inhibit PDE4. In vitro studies indicate that most of the synthesized compounds show significant potency for the inhibition of PDE4. Specifically, N-(4-(3-(3,5-dimethoxyphenyl)-1H-pyrazol-5-yl)benzyl)-2-morpholinoethan-1-amine exhibits the most potent PDE4 inhibition, with an IC50 value of ca. 0.09 µM. It also produces antidepressant-like activities in sugar water consumption and in forced swimming tests in vivo. [ABSTRACT FROM AUTHOR] |
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| قاعدة البيانات: |
Complementary Index |
