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1,3,4-恶二唑、1,3,4-噻二唑和1,2,4-三唑的合成、抗菌及细胞毒性活性

Synthesis, antimicrobial and cytotoxic activities of 1,3,4-oxadiazoles, 1,3,4-thiadiazoles and 1,2,4-triazoles.

作者信息

Padmavathi V, Sudhakar Reddy G, Padmaja A, Kondaiah P

机构信息

Department of Chemistry, Sri Venkateswara University, Tirupati 517 502, Andhra Pradesh, India.

出版信息

Eur J Med Chem. 2009 May;44(5):2106-12. doi: 10.1016/j.ejmech.2008.10.012. Epub 2008 Nov 1.

Abstract

A new class of 1,3,4-oxadiazoles were prepared from acid hydrazides on treatment with different carboxylic acids in the presence of phosphorus oxychloride. Interconversion of oxadiazoles to thiadiazoles and triazoles was carried out with appropriate reagents. The antimicrobial and cytotoxic activities of compounds 7a-d to 12a-d were tested. Compounds 10d and 12d showed pronounced antimicrobial activity. Further, compound 10d exhibited maximum cytotoxicity.

摘要

通过酰肼在三氯氧磷存在下与不同的羧酸反应制备了一类新型的1,3,4-恶二唑。用适当的试剂实现了恶二唑向噻二唑和三唑的相互转化。测试了化合物7a-d至12a-d的抗菌和细胞毒性活性。化合物10d和12d表现出显著的抗菌活性。此外,化合物10d表现出最大的细胞毒性。

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