The State of the Art of Pyrazole Derivatives as Monoamine Oxidase Inhibitors and Antidepressant/Anticonvulsant Agents

被引:116
作者
Secci, D. [1 ]
Bolasco, A. [1 ]
Chimenti, P. [1 ]
Carradori, S. [1 ]
机构
[1] Univ Roma La Sapienza, Dipartimento Chim & Tecnol Farmaco, I-00185 Rome, Italy
关键词
Alzheimer's disease; anticonvulsant agents; antidepressant agents; isocarboxazid; monoamine oxidase; Parkinson's disease; Porsolt's Test; pyrazole; pyrazolidine; pyrazoline; N-thiocarbamoyl; ANTIDEPRESSANT ACTIVITY; 1-N-SUBSTITUTED THIOCARBAMOYL-3-PHENYL-5-THIENYL-2-PYRAZOLINES; 1-ACETYL-3,5-DIPHENYL-4,5-DIHYDRO-(1H)-PYRAZOLE DERIVATIVES; ANTICONVULSANT ACTIVITIES; BIOLOGICAL EVALUATION; B INHIBITORS; ANIMAL-MODEL; MAO; ANXIETY; POTENT;
D O I
10.2174/092986711797636090
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
070307 [化学生物学]; 071010 [生物化学与分子生物学];
摘要
Monoamine oxidase plays a significant role in the control of intracellular concentration of monoaminergic neurotransmitters or neuromodulators and dietary amines. The rapid degradation of these molecules ensures the proper functioning of synaptic neurotransmission and is critically important for the regulation of emotional and other brain functions. The development of human MAO inhibitors led to important breakthroughs in the therapy of several neuropsychiatric disorders. Different families of heterocycles containing 2 or 4 nitrogen atoms have been used as scaffolds for synthesizing selective monoamine oxidase inhibitors, but the early period of the MAO-inhibitors started with hydrazine derivatives. Pyrazole, pyrazoline, and pyrazolidine derivatives can be considered as a cyclic hydrazine moiety. This scaffold also displayed promising antidepressant and anticonvulsant properties as demonstrated by different and established animal models. Diversely substituted pyrazoles, embedded with a variety of functional groups, are important biological agents and a significant amount of research activity has been directed towards this chemical class.
引用
收藏
页码:5114 / 5144
页数:31
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