Design, synthesis and potential 6 Hz psychomotor seizure test activity of some novel 2-(substituted)-3-{(substituted)amino}quinazolin-4(3H)-one.

Kumar P; Shrivastava B; Pandeya SN; Stables JP

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Design, synthesis and potential 6 Hz psychomotor seizure test activity of some novel 2-(substituted)-3-{(substituted)amino}quinazolin-4(3H)-one.

机译：一些新型2-（取代）-3-{（取代）氨基}喹唑啉-4（3H）-一的设计，合成和潜在的6 Hz精神运动性癫痫发作试验活性。

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Thirty new 2-(substituted)-3-{[substituted]amino}quinazolin-4(3H)-one were designed and synthesized keeping in view the structural requirement of pharmacophore and evaluated for anticonvulsant activity and neurotoxicity. The anticonvulsant activity of the titled compounds was assessed using the 6 Hz psychomotor seizure test. The most active compound of the series was 3-({(E)-[3-(4-chloro-3-methylphenoxy)phenyl]methylidene}amino)-2-phenylquinazolin -4(3H)-one PhQZ 7, which showed 100% protection (4/4, 0.5 h) and 75% protection (3/4, 0.25 h) at a dose of 100 mg/kg in mice. A computational study was carried out for calculation of pharmacophore pattern and prediction of pharmacokinetic properties. Titled compounds have also exhibited good binding properties with epilepsy molecular targets such as glutamate, GABA (A) delta and GABA (A) alpha-1 receptors, in Lamarckian genetic algorithm based flexible docking studies.

机译：考虑到药效团的结构要求，设计并合成了三十种新的2-（取代的）-3-{[取代的]氨基}喹唑啉-4（3H）-，并评价了其抗惊厥活性和神经毒性。使用6Hz精神运动性癫痫发作测试评估标题化合物的抗惊厥活性。该系列中活性最高的化合物是3-（{（E）-[3-（4-氯-3-甲基苯氧基）苯基]亚甲基}氨基）-2-苯基喹唑啉-4（3H）-一个PhQZ 7，在小鼠中以100 mg / kg的剂量提供100％保护（4/4，0.5 h）和75％保护（3/4，0.25 h）。进行了计算研究，以计算药效团模式和预测药代动力学特性。在基于Lamarckian遗传算法的灵活对接研究中，标题化合物还具有与癫痫分子靶标（例如谷氨酸，GABA（A）δ和GABA（A）α-1受体）的良好结合特性。

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《European Journal of Medicinal Chemistry: Chimie Therapeutique》 |2011年第4期|共13页
作者
Kumar P; Shrivastava B; Pandeya SN; Stables JP;
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1. Design, synthesis and potential 6 Hz psychomotor seizure test activity of some novel 2-(substituted)-3-{(substituted)amino}quinazolin-4(3H)-one. [J] . Kumar P, Shrivastava B, Pandeya SN, European Journal of Medicinal Chemistry: Chimie Therapeutique . 2011,第4期

机译：一些新型2-（取代）-3-{（取代）氨基}喹唑啉-4（3H）-一的设计，合成和潜在的6 Hz精神运动性癫痫发作试验活性。
2. Design and synthesis of 3-(4-chlorophenyl)-2-(2-(4-substituted)-2-oxoethylthio)quinazolin-4(3H)-one as antihistamine agents [J] . V. Alagarsamy, B. Narendhar, M. T. Sulthana, Medicinal chemistry research: an international journal for rapid communications on design and mechanisms of action of biologically active agents . 2014,第11期

机译：抗组胺药3-（4-氯苯基）-2-（2-（4-取代）-2-氧乙硫基）喹唑啉-4（3H）-one的设计与合成
3. A New Class of Anticonvulsants Possessing 6 Hz Psychomotor Seizure Test Activity: 2-(1H-Benzotriazol-1-yl)-N'-[Substituted] Acetohydrazides. [J] . Praveen Kumar, Laxmi Tripathi Medicinal chemistry . 2012,第3期

机译：具有6 Hz精神运动性癫痫发作试验活动的新型抗惊厥药：2-（1H-苯并三唑-1-基）-N'-[取代]乙酰肼。
4. Synthesis of 2-((4-Substituted Phenyl) Amino) Benzaldehyde [C] . Yongli Duan, Zhimin Li, Qidong Tang, International Conference on Electronics, Mechanics, Culture and Medicine . 2017

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5. Development of synthetic approaches towards 2- substituted 3- and 4-fluorothiophene building blocks and their application in liquid crystal synthesis. [D] . Subramanian, Pritha. 2013

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机译：3-（取代的）-2-（4-氧代-2-苯基喹唑啉-3（4H）-氨基氨基）喹唑啉-4（3H）-的合成及抑菌活性
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Design, synthesis and potential 6 Hz psychomotor seizure test activity of some novel 2-(substituted)-3-{(substituted)amino}quinazolin-4(3H)-one.

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