Li, Shengke published the artcileSupramolecular Modulation of Antibacterial Activity of Ambroxol by Cucurbit[7]uril, Application of trans-4-((2-Amino-3,5-dibromobenzyl)amino)cyclohexanol hydrochloride, the publication is ChemPlusChem (2020), 85(4), 679-683, database is CAplus and MEDLINE.
Supramol. encapsulation by cucurbit[7]uril (CB[7]) was recently demonstrated to provide a simple and efficient method for antibacterial activity regulation of antibiotics. In this work, CB[7] was shown to form binary host-guest complex with ambroxol hydrochloride (ABX), a clin. mucokinetic and expectorant drug, which was reported to exhibit certain antibacterial activity. 1H NMR titration and isothermal titration calorimetry experiment results suggested that the 4-hydroxyl cyclohexylamine group of ABX was included inside the CB[7] cavity, with a binding constant Ka of (6.69±0.11)×105 M-1 in phosphate buffered saline (PBS) solution, thermodynamically driven by both enthalpy change and entropy. More importantly, ABX’s inhibitory activity (MIC50) against bacillary strains towards Pseudomonas aeruginosa and Escherichia coli strains was decreased from (5.11±0.31)×10-6 M-1 and (2.63±0.34)×10-5 M-1 to zero upon encapsulation by CB[7], and was subsequently recovered to almost its original activity when a competitive guest, amantadine hydrochloride, for disassembling CB[7]-ABX complex, was added, suggesting that the antibacterial activity of ABX could be readily “turned off/on” upon its complexation and decomplexation with CB[7].
ChemPlusChem published new progress about 23828-92-4. 23828-92-4 belongs to alcohols-buliding-blocks, auxiliary class Membrane Transporter/Ion Channel,Sodium Channel, name is trans-4-((2-Amino-3,5-dibromobenzyl)amino)cyclohexanol hydrochloride, and the molecular formula is C13H19Br2ClN2O, Application of trans-4-((2-Amino-3,5-dibromobenzyl)amino)cyclohexanol hydrochloride.
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