Synthesis and in vitro antimycobacterial activity of 8-OCH3 ciprofloxacin methylene and ethylene isatin derivatives was written by Feng, Lian-Shun;Liu, Ming-Liang;Zhang, Shu;Chai, Yun;Wang, Bo;Zhang, Yi-Bin;Lv, Kai;Guan, Yan;Guo, Hui-Yuan;Xiao, Chun-Ling. And the article was included in European Journal of Medicinal Chemistry in 2010.Formula: C18H20FN3O4 This article mentions the following:
A series of novel 8-OCH3 ciprofloxacin methylene and ethylene isatin derivatives with remarkable improvement in lipophilicity were synthesized in this study. These derivatives were evaluated for their in vitro activity against some mycobacteria. All of the synthesized compounds were less active than the parent 8-OCH3 ciprofloxacin against Mycobacterium smegmatis CMCC 93202, but most of the methylene isatin derivatives were more active than 8-OCH3 ciprofloxacin, ciprofloxacin, isoniazid and rifampin against MTB H37Rv ATCC 27294. It was noted that compound I (MIC: 0.074 μM) was 2-13 fold more potent than the reference compounds against MTB H37Rv ATCC 27294, and some compounds (MIC: 6.72-7.05 μM) were around 1.6 fold more potent than the parent 8-OCH3 ciprofloxacin, 3.5 fold more potent than ciprofloxacin against MDR-MTB 09710. In the experiment, the researchers used many compounds, for example, 1-Cyclopropyl-6-fluoro-8-methoxy-4-oxo-7-(piperazin-1-yl)-1,4-dihydroquinoline-3-carboxylic acid (cas: 112811-57-1Formula: C18H20FN3O4).
1-Cyclopropyl-6-fluoro-8-methoxy-4-oxo-7-(piperazin-1-yl)-1,4-dihydroquinoline-3-carboxylic acid (cas: 112811-57-1) belongs to piperazine derivatives. A form in which piperazine is commonly available industrially is as the hexahydrate, C4H10N2. 6H2O, which melts at 44 °C and boils at 125–130 °C. Piperazine is an anthelminthic especially useful in the treatment of partial intestinal obstruction caused by Ascaris worms, which is a condition primarily seen in children. Piperazine hydrate and piperazine citrate are the main anthelminthic piperazines.Formula: C18H20FN3O4
Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics