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新型N-亚糠基和N-亚苯乙酰基-5-氯二苯胺-2-羧酸酰肼作为抗病毒和抗菌剂的合成

Synthesis of newer N-furylidene and N-acetophenonylidene-5-chlorodiphenylamine-2-carboxylic acid hydrazides as antiviral and antibacterial agents.

作者信息

Bahadur S, Singh S P

出版信息

Pharmazie. 1980 Aug;35(8):463-5. doi: 10.1002/chin.198050198.

DOI:10.1002/chin.198050198
PMID:6776544
Abstract

Five N-furylidene and fifteen N-acetophenonylidene-5-chlorodiphenylamine-2-carboxylic acid hydrazides were synthesized by the condensation of 5-chlorodiphenylamine-2-carboxylic acid hydrazides with furfuraldehyde and appropriate acetophenones. All the N-acetophenonylidenes thus synthesized were screened for their antiviral activity against animal viruses (Ranikhet disease virus and vaccinia virus in a stationary culture of chorioallantoic membrane of chick embryo) and against plant virus, namely gomphrena mosaic virus (GMV) in vitro as well as in vivo. Whereas five N-furylidenes were tested against gomphrena mosaic virus only in vitro and in vivo for their antiviral activity. Maximum significant protection was observed to the extent of 20% against Ranikhet disease virus. The majority of these compounds showed highly significant antiviral activity up to the extent of 96% in vitro and 89% in vivo against gomphrena mosaic virus. These compounds were also screened for their antibacterial activity against two micro-organisms; Bacillus subtilis and Staphylococcus aureus. Almost all of them were found to exhibit significant inhibition against B. subtilis while only a fewer showed significant inhibition against S. aureus.

摘要

通过5-氯二苯胺-2-羧酸酰肼与糠醛及相应的苯乙酮缩合,合成了5种N-亚糠基和15种N-亚苯乙酰基-5-氯二苯胺-2-羧酸酰肼。对所有由此合成的N-亚苯乙酰基化合物针对动物病毒(鸡胚绒毛尿囊膜静止培养中的新城疫病毒和痘苗病毒)以及植物病毒即千日红花叶病毒(GMV)进行了体外和体内抗病毒活性筛选。而5种N-亚糠基化合物仅在体外和体内针对千日红花叶病毒测试了其抗病毒活性。观察到对新城疫病毒有高达20%的最大显著保护作用。这些化合物中的大多数对千日红花叶病毒在体外表现出高达96%、在体内表现出高达89%的高度显著抗病毒活性。还对这些化合物针对两种微生物即枯草芽孢杆菌和金黄色葡萄球菌的抗菌活性进行了筛选。几乎所有化合物都对枯草芽孢杆菌表现出显著抑制作用,而只有少数对金黄色葡萄球菌表现出显著抑制作用。

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