Novel Organic Salts Based on Mefloquine: Synthesis, Solubility, Permeability, and In Vitro Activity against Mycobacterium tuberculosis was written by Silva, Dario;Lopes, Marcio V. C.;Petrovski, Zeljko;Santos, Miguel M.;Santos, Jussevania P.;Yamada-Ogatta, Sueli F.;Bispo, Marcelle L. F.;de Souza, Marcus V. N.;Duarte, Ana Rita C.;Lourenco, Maria C. S.;Goncalves, Raoni Schroeder B.;Branco, Luis C.. And the article was included in Molecules in 2022.Product Details of 75277-39-3 This article mentions the following:
The development of novel pharmaceutical tools to efficiently tackle tuberculosis is the order of the day due to the rapid development of resistant strains of Mycobacterium tuberculosis. Herein, we report novel potential formulations of a repurposed drug, the antimalarial mefloquine (MFL), which was combined with organic anions as chem. adjuvants. Eight mefloquine organic salts were obtained by ion metathesis reaction between mefloquine hydrochloride ([MFLH][Cl]) and several organic acid sodium salts in high yields. One of the salts, mefloquine mesylate ([MFLH][MsO]), presented increased water solubility in comparison with [MFLH][Cl]. Moreover, all salts with the exception of mefloquine docusate ([MFLH][AOT]) showed improved permeability and diffusion through synthetic membranes. Finally, in vitro activity studies against Mycobacterium tuberculosis revealed that these ionic formulations exhibited up to 1.5-times lower MIC values when compared with [MFLH][Cl], particularly mefloquine camphorsulfonates ([MFLH][(1R)-CSA], [MFLH][(1S)-CSA]) and mefloquine HEPES ([MFLH][HEPES]). In the experiment, the researchers used many compounds, for example, Sodium 2-(4-(2-hydroxyethyl)piperazin-1-yl)ethanesulfonate (cas: 75277-39-3Product Details of 75277-39-3).
Sodium 2-(4-(2-hydroxyethyl)piperazin-1-yl)ethanesulfonate (cas: 75277-39-3) belongs to piperazine derivatives. Simple N-substituted piperazines have been found in many drug molecules. Piperazine is formed as a co-product in the ammoniation of 1,2-dichloroethane or ethanolamine. These are the only routes to the chemical used commercially.Product Details of 75277-39-3
Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics