- Synthesis of sulfur-containing cationic lipids of the 1,3-dioxolane type
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A series of cationic acetal lipids containing different spacer and cationic groups were synthesized starting from 1,2-O-hexadecylidene-3-thioglycerol.
- Klykov,Serebrennikova
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- PHARMACEUTICAL COMPOSITIONS OF LIPOIC ACID CHOLINE ESTER SALTS AND METHODS OF TREATMENT USING SAME
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The present disclosure provides salts of lipoic acid choline ester (LACE), crystalline forms thereof, and methods of use thereof. The present disclosure further provides pharmaceutical compositions of LACE salts and methods of use thereof.
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Page/Page column 71-72
(2021/09/17)
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- Synthesis, physicochemical properties and biological activities of novel alkylphosphocholines with foscarnet moiety
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A series of alkylphosphocholines with foscarnet moiety was synthesized. The structure of these zwitterionic amphiphiles was modified in both polar and non-polar parts of surfactant molecule. Investigations of physicochemical properties are represented by the determination of critical micelle concentration, the surface tension value at the cmc and the surface area per surfactant head group utilising surface tension measurements. Hydrodynamic diameter of surfactant micelles was determined using the dynamic light scattering technique. Alkylphosphocholines exhibit significant cytotoxic, anticandidal (Candida albicans) and antiamoebal (Acanthamoeba spp. T4 genotype) activity. The relationship between the structure, physicochemical properties and biological activity of the tested compounds revealed that lipophilicity has a significant influence on biological activity of the investigated surfactants. More lipophilic alkylphosphocholines with octadecyl chains show cytotoxic activity against cancer cells which is higher than that of the compounds with shorter alkyl chains. The opposite situation was observed in case of anticandidal and antiamoebal activity of these surfactants. The most active compounds were found to have pentadecyl chains. The foscarnet analogue of miltefosine C15-PFA-C showed the highest anticandidal activity. The minimum value of anticandidal activity of this compound is 1,4 μM thus representing the highest anticandidal activity found within the group of alkylphosphocholines.
- Mrva, Martin,Bukovsky, Marián,Devínsky, Ferdinand,Garajová, Mária,Juhásová, Anna,Luká?, Milo?,Moj?i?, Ján,Moj?i?ová, Gabriela,Pisár?ik, Martin,Timko, Luká?
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- Environment-friendly choline ionic liquid and preparation method therefor
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The invention relates to environment-friendly novel choline ionic liquid and a method for preparing the choline ionic liquid. The novel choline ionic liquid contains levulinic acid choline, sorbic acid choline, glutaric acid choline, adipic acid choline, (p-, m- and o-)phthalic acid choline, trifluoromethanesulfonic acid choline, benzenesulfonic acid choline, (p-, m- and o-)toluenesulfonic acid choline, bis(trifluoromethane sulfonimide) choline and the like. The novel choline ionic liquid has the remarkable advantages that the preparation process is simple, the recovery is simple and convenient, the stability of reuse is good, and the like.
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Paragraph 0031; 0032; 0033; 0034; 0035; 0036
(2016/10/20)
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- The silane compound surface modification material phosphorylcholine-
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PROBLEM TO BE SOLVED: To provide a novel compound serving as a surface modifying material for a high sensitivity biosensing element, which enables forming of a monomolecular film capable of inhibiting nonspecific adsorption of protein. SOLUTION: The compound is a phosphorylcholine-silane compound represented by chemical formula 1, wherein X1to X3each independently represent halogen, 1-3C alkoxy or 1-3C alkyl, provided that at least one of X1to X3is halogen or 1-3C alkoxy; R1represents -(CH2)m- or -(CH2CH2O)n-(CH2)2-; R2represents -(CH2)s- or -(CH2)3-(OCH2CH2)p-; m is an integer of 2-20, n is an integer of 1-5, s is an integer of 3-20, and p is an integer of 1-5. COPYRIGHT: (C)2013,JPOandINPIT
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Paragraph 0017
(2018/06/29)
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- Synthesis of phosphorylcholine-oligoethylene glycol-alkane thiols and their suppressive effect on non-specific adsorption of proteins
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A series of phosphorylcholine-oligoethylene glycol-alkane thiols were synthesized, and their suppressive effect on the non-specific adsorption of proteins was evaluated by comparison with corresponding oligoethylene glycol-alkane thiols. It was found that
- Tanaka, Mutsuo,Sawaguchi, Takahiro,Sato, Yukari,Yoshioka, Kyoko,Niwa, Osamu
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supporting information; experimental part
p. 4092 - 4095
(2009/12/01)
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- Dialkylamino and nitrogen heterocyclic analogues of hexadecylphosphocholine and cetyltrimetylammonium bromide: Effect of phosphate group and environment of the ammonium cation on their biological activity
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A series of dialkylamino and nitrogen heterocyclic analogues of hexadecylphosphocholine and cetyltrimethylammonium bromide have been synthesized. The prepared compounds exhibit significant cytotoxic, antifungal and antiprotozoal activities. Alkylphosphocholines possess higher antifungal activity against Candida albicans in comparison with quaternary ammonium compounds. However, quaternary ammonium compounds exhibit significant higher activity against human tumor cells and Acanthamoeba lugdunensis compared to alkylphosphocholines. In addition, their haemolytic toxicity has been investigated. The relationship between structure and biological activity of the tested compounds is discussed.
- Lukac, Milos,Mojzis, Jan,Mojzisova, Gabriela,Mrva, Martin,Ondriska, Frantisek,Valentova, Jindra,Lacko, Ivan,Bukovsky, Marian,Devinsky, Ferdinand,Karlovska, Janka
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experimental part
p. 4970 - 4977
(2010/02/27)
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