Synthesis and local anesthetic activity of some novel N-(5-(4-Substituted)phenyl-1,3,4-oxadiazol-2-yl)-2-(substituted)-acetamides.

Rajak H; Kharya MD; Mishra P

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Synthesis and local anesthetic activity of some novel N-(5-(4-Substituted)phenyl-1,3,4-oxadiazol-2-yl)-2-(substituted)-acetamides.

机译：一些新型N-（5-（4-取代）苯基-1,3,4-恶二唑-2-基）-2-（取代）-乙酰胺的合成及局部麻醉活性。

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A novel series of acetamides carrying substituted-1,3,4-oxadiazole moiety were synthesized from reaction of 5-aryl-2-chloroacetamido-1,3,4-oxadiazoles with different secondary amines. The local anesthetic potential of the compounds was investigated using rabbit corneal reflex method and guinea pig's wheal derm method. The present work is the only one of its kind reporting local anesthetic activity in acetamide system combined with 1,3,4-oxadiazole nucleus. Lidocaine was selected as standard drug in evaluation of local anesthetic activity of synthesized oxadiazole analogues. Compound 19 was found to possess significant local anesthetic activity in both the models employed for evaluation of local anesthetic activity. Compound 20, 23, 28, 29 and 35 also demonstrated marked local anesthetic activities. Structure-activity relationships among synthesized compounds were also established.

机译：由5-芳基-2-氯乙酰胺基-1,3,4-恶二唑与不同的仲胺反应合成了一系列带有取代的1,3,4-恶二唑部分的新型乙酰胺。使用兔角膜反射法和豚鼠的风皮法研究了这些化合物的局部麻醉潜力。目前的工作是该类中唯一一种在乙酰胺系统中结合1,3,4-恶二唑核的局部麻醉活性的研究。选择利多卡因作为标准药物，以评估合成的恶二唑类似物的局部麻醉活性。在用于评估局部麻醉活性的两个模型中，发现化合物19都具有显着的局部麻醉活性。化合物20、23、28、29和35也显示出明显的局部麻醉活性。还建立了合成化合物之间的构效关系。

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《Archiv der Pharmazie》 |2008年第4期|共15页
作者
Rajak H; Kharya MD; Mishra P;
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正文语种 eng
中图分类药学;
关键词
Local Anesthetics; novel; Synthesis; Evaluation;

机译：局麻;新颖;合成;评价;

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1. Synthesis and local anesthetic activity of some novel N-(5-(4-Substituted)phenyl-1,3,4-oxadiazol-2-yl)-2-(substituted)-acetamides. [J] . Rajak H, Kharya MD, Mishra P Archiv der Pharmazie . 2008,第4期

机译：一些新型N-（5-（4-取代）苯基-1,3,4-恶二唑-2-基）-2-（取代）-乙酰胺的合成及局部麻醉活性。
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Synthesis and local anesthetic activity of some novel N-(5-(4-Substituted)phenyl-1,3,4-oxadiazol-2-yl)-2-(substituted)-acetamides.

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