Category: 112811-57-1

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

Desirability-Based Methods of Multiobjective Optimization and Ranking for Global QSAR Studies. Filtering Safe and Potent Drug Candidates from Combinatorial Libraries was written by Cruz-Monteagudo, Maykel;Borges, Fernanda;Cordeiro, M. Natalia D. S.;Cagide Fajin, J. Luis;Morell, Carlos;Molina Ruiz, Reinaldo;Canizares-Carmenate, Yudith;Dominguez, Elena Rosa. And the article was included in Journal of Combinatorial Chemistry in 2008.SDS of cas: 112811-57-1 This article mentions the following:

Up to now, very few applications of multiobjective optimization (MOOP) techniques to quant. structure-activity relationship (QSAR) studies have been reported in the literature. However, none of them report the optimization of objectives related directly to the final pharmaceutical profile of a drug. In this paper, a MOOP method based on Derringer’s desirability function that allows conducting global QSAR studies, simultaneously considering the potency, bioavailability, and safety of a set of drug candidates, is introduced. The results of the desirability-based MOOP (the levels of the predictor variables concurrently producing the best possible compromise between the properties determining an optimal drug candidate) are used for the implementation of a ranking method that is also based on the application of desirability functions. This method allows ranking drug candidates with unknown pharmaceutical properties from combinatorial libraries according to the degree of similarity with the previously determined optimal candidate. Application of this method will make it possible to filter the most promising drug candidates of a library (the best-ranked candidates), which should have the best pharmaceutical profile (the best compromise between potency, safety and bioavailability). In addition, a validation method of the ranking process, as well as a quant. measure of the quality of a ranking, the ranking quality index (Ψ), is proposed. The usefulness of the desirability-based methods of MOOP and ranking is demonstrated by its application to a library of 95 fluoroquinolones, reporting their gram-neg. antibacterial activity and mammalian cell cytotoxicity. Finally, the combined use of the desirability-based methods of MOOP and ranking proposed here seems to be a valuable tool for rational drug discovery and development. 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: 112811-57-1SDS of cas: 112811-57-1).

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. Piperazine was first introduced as an anthelmintic in 1953. Piperazine compounds mediate their anthelmintic action by generally paralyzing parasites, allowing the host body to easily remove or expel the invading organism. Intermediate for a wide range of pharmaceuticals, polymers, dyes, corrosion inhibitors, rubber accelerators and surfactants.SDS of cas: 112811-57-1

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Synthesis of pyrazinamide Mannich bases and their antitubercular properties was written by Sriram, Dharmarajan;Yogeeswari, Perumal;Reddy, Sushma Pobba. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2006.Recommanded Product: 112811-57-1 This article mentions the following:

A series of pyrazinamide (PAZ) Mannich bases has been synthesized by reacting PAZ, formaldehyde, and various substituted piperazines using microwave irradiation with the yield ranging from 46% to 86%. The synthesized compounds were evaluated for antimycobacterial activity in vitro and in vivo against Mycobacterium tuberculosis H37Rv (MTB). Among the synthesized compounds, 1-cyclopropyl-6-fluoro-1,4-dihydro-8-methoxy-7-(3-methyl-4-((pyrazine-2-carboxamido)methyl)piperazinyl)-4-(oxo)-3-quinoline-carboxylic acid (I) was found to be the most active compound in vitro with MIC of 0.39 and 0.2 μg/mL against MTB and multidrug-resistant MTB, resp. In the in vivo animal model I decreased the bacterial load in lung and spleen tissues with 1.86 and 1.66-log10 protections, resp. 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: 112811-57-1Recommanded Product: 112811-57-1).

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. Industrial applications of piperazine include the manufacture of plastics, resins, pesticides and brake fluids. Intermediate for a wide range of pharmaceuticals, polymers, dyes, corrosion inhibitors, rubber accelerators and surfactants.Recommanded Product: 112811-57-1

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics