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新型 4,6-二取代 3(2H)-哒嗪酮-乙酰腙衍生物的合成及体外生物活性。

Synthesis and in vitro biological activity of new 4,6-disubstituted 3(2H)-pyridazinone-acetohydrazide derivatives.

机构信息

Gazi University, Faculty of Pharmacy, Department of Pharmaceutical Chemistry, 06330 Ankara, Turkey.

出版信息

Z Naturforsch C J Biosci. 2012 May-Jun;67(5-6):257-65.

Abstract

New 3(2H)-pyridazinone derivatives containing a N'-benzyliden-acetohydrazide moiety at position 2 were synthesized. The structures of these newly synthesized compounds were confirmed by IR, 1H NMR, and MS data. These compounds were tested for their antibacterial, antifungal, antimycobacterial, and cytotoxic activities. The compounds 2-[4-(4-chlorophenyl)-6-(morpholin-4-yl)-3-oxo-(2H)-pyridazin-2-yl]-N'-(4-tert-butylbenzyliden)acetohydrazide and 2-[4-(4-chlorophenyl)-6-(morpholin-4-yl)-3-oxo-(2H)-pyridazin-2-yl]-N'-(4-chlorobenzyliden) acetohydrazide exhibited activity against both Gram-positive and Gram-negative bacteria. Most of the compounds were active against E. coli ATCC 35218. The preliminary results of this study revealed that some target compounds exhibited promising antimicrobial activities.

摘要

合成了 2 位含有 N'-苄叉基乙二酰腙部分的新型 3(2H)-哒嗪酮衍生物。这些新合成化合物的结构通过 IR、1H NMR 和 MS 数据得到确认。这些化合物被测试了其抗菌、抗真菌、抗分枝杆菌和细胞毒性活性。化合物 2-[4-(4-氯苯基)-6-(吗啉-4-基)-3-氧代-(2H)-哒嗪-2-基]-N'-(4-叔丁基苄叉基)乙二酰腙和 2-[4-(4-氯苯基)-6-(吗啉-4-基)-3-氧代-(2H)-哒嗪-2-基]-N'-(4-氯苄叉基)乙二酰腙对革兰氏阳性菌和革兰氏阴性菌均具有活性。大多数化合物对大肠杆菌 ATCC 35218 具有活性。本研究的初步结果表明,一些目标化合物表现出有希望的抗菌活性。

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