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设计并合成新型二苯甲酰胺和二苯乙酰胺衍生物作为抗惊厥药物。

Design and synthesis of novel diphenyl oxalamide and diphenyl acetamide derivatives as anticonvulsants.

机构信息

Department of Pharmaceutical Chemistry, Y.B. Chavan College of Pharmacy, Aurangabad (M.S.), India.

出版信息

Arch Pharm (Weinheim). 2012 Jan;345(1):57-64. doi: 10.1002/ardp.201100108. Epub 2011 Sep 23.

Abstract

A series of novel N(1) -substituted-N(2) ,N(2) -diphenyl oxalamides 3a-l were synthesized in good yield by stirring diphenylcarbamoyl formyl chloride (2) and various substituted aliphatic, alicyclic, aromatic, heterocyclic amines in DMF and K(2) CO(3) . Also 2-substituted amino-N,N-diphenylacetamides 5a-m were designed by pharmacophore generation and synthesized by stirring 2-chloro-N,N-diphenylacetamide (4) and various substituted amines in acetone using triethyl amine as a catalyst. All the synthesized compounds were screened for anticonvulsant activity in Swiss albino mice by MES and ScPTZ induced seizure tests. Neurotoxicity screening and behavioral testing was also carried out. Some of the synthesized test compounds were found to be more potent than the standard drug.

摘要

一系列新型 N(1)-取代-N(2),N(2)-二苯基草酰胺 3a-l 通过搅拌二苯甲酰基甲酰胺基氯 (2) 和各种取代的脂肪族、脂环族、芳香族、杂环胺在 DMF 和 K2CO3 中以高产率合成。此外,通过搅拌 2-氯-N,N-二苯乙酰胺 (4) 和各种取代的胺在丙酮中用三乙胺作为催化剂,通过药效团生成设计了 2-取代的氨基-N,N-二苯乙酰胺 5a-m。所有合成的化合物均通过 MES 和 ScPTZ 诱导的惊厥试验在瑞士白化小鼠中进行抗惊厥活性筛选。还进行了神经毒性筛选和行为测试。一些合成的测试化合物比标准药物更有效。

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