- Nonionic Isatin Surfactants: Synthesis, Quantum Chemical Calculations, ADMET and Their Antimicrobial Activities
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The most challenge task in the building up of surface-active molecules is maximizing their surface activity with good biological activity. A nonionic surfactant (N-isatin-EOm-Cn where m is 5, 7 and 9 ethylene glycol units and n is 8, 10 and 12) is achieved by first reacting isatin with chloroacetic acid and then with different types of ethoxylated (C8–C12) fatty alcohols that possess 5, 7 and 9 ethylene oxide units. The prepared surfactants were characterized by FTIR and 1H NMR to confirm the structure. The surface activity, biodegradability, antimicrobial, and antifungal activity of the surfactants were evaluated. In addition, quantum chemical calculations and computations of oral bioavailability were performed. The obtained data show that all the synthesized compounds had good surface activity, biodegradability and biological activity.
- Hussein, Ahmed M.,Khowdiary, Manal M.
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p. 489 - 501
(2020/02/11)
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- Application of Monodisperse PEGs in Pharmaceutics: Monodisperse Polidocanols
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Polydisperse PEGs are ubiquitously used in pharmaceutical industry and biomedical research. However, the monodispersity in PEGs may play a role in the development of safe and effective PEGylated small molecular drugs. Here, to avoid the polydispersity in polidocanol, the active ingredient in a clinically used drug, a macrocyclic sulfate-based strategy for the efficient and scalable synthesis of monodisperse polidocanols, their sulfates, and their methylated derivatives, was developed. TLC and HPLC analysis indicated a complex mixture in regular polidocanol and high purities in monodisperse polidocanols and their derivatives. Assay on HUVEC, L929, and HePG2 cells showed that monodisperse polidocanols have much higher cytotoxicity and safety than that of regular polidocanol. It was found that the monodispersity of PEGs in polidocanols is crucial for achieving the optimal therapeutic results. Therefore, based on this case study, it would be beneficial to optimize PEGylated small molecular drugs with monodisperse PEGs in pharmaceutical research and development.
- Yu, Zeqiong,Bo, Shaowei,Wang, Huiyuan,Li, Yu,Yang, Zhigang,Huang, Yongzhuo,Jiang, Zhong-Xing
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p. 3473 - 3479
(2017/10/11)
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- Preparation method and application of monodisperse nonapolyethylene glycol dodecyl alcohol monoether and sulphate thereof
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The invention discloses a preparation method and application of monodisperse nonapolyethylene glycol dodecyl alcohol monoether and sulphate thereof and belongs to the field of pharmaceutical and chemical industry. Starting from dodecyl alcohol, firstly ring-opening reaction is carried out with nonapolyethylene glycol cyclic sulphate once or with multiple oligomeric ethylene glycol cyclic sulphate containing nine ethylene glycol units in total for multiple times in presence of alkali, so that sulphate of nonapolyethylene glycol dodecyl alcohol monoether is obtained; and then hydrolysis is carried out in presence of sulphuric acid, so that the nonapolyethylene glycol dodecyl alcohol monoether is obtained. The preparation method can be applied to preparation of long-chain alkyl monoether of monodisperse polyethylene glycol and sulphate thereof. The preparation method disclosed by the invention has the advantages that single molecular weight polyethylene glycol cyclic sulphate is taken as a raw material, efficient synthesis of more than hexameric alkyl alcohol monoether of ethylene glycol is realized, no protecting group is used during synthesis, steps are simple and convenient, the preparation method is applicable to industrial production, and the obtained product has obvious advantages compared with existing prepared lauromacrogol.
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- Nonionic surfactant having reduced toxicity and environmental hormone activity and preperation method of the same
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The present invention relates to a non-ionic surfactant with reduced toxicity and activity of endocrine-disrupting chemicals, and to a preparation method thereof. According to the present invention, the non-ionic surfactant exhibits characteristics of remarkably reducing toxicity and effects on the survival of cells, and exhibits inactiveness of endocrine-disrupting chemicals, thereby being useful as a surfactant replacing a conventional surfactant such as NPEs, and the like. Particularly, the non-ionic surfactant is useful as a cleaning composition, a fabric softener composition, a cosmetic composition, an emulsifier composition, a dispersant composition, and the like.
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Paragraph 0157-0159
(2017/06/13)
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- PHOSPHOLIPID-DETERGENT CONJUGATES AND USES THEREOF
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The invention relates to novel compounds, in particular novel O-substituted phospholipids that are useful for the in vitro and in vivo delivery of drugs as well as nucleic acids into cells. The invention also relates to pharmaceutical compositions and supramolecular complexes comprising said compounds and the use of these compounds in therapeutic treatment, in particular in gene therapy.
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Page/Page column 79; 80
(2013/03/26)
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- Combinatorial synthesis of PEG oligomer libraries
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A simple chain-extending approach was established for the scale-up of the monoprotected monodisperse PEG diol materials. Reactions of THP-(OCH2CH2)n—OMs (n=4, 8, 12) with a large excess of commercially available H—(OCH2CH2)n—OH (n=1-4) under basic conditions led to THP-(OCH2CH2)n—OH (n=5-15). Similarly, Me-(OCH2CH2)n—OH (n=4-11, 13) were prepared from Me-(OCH2CH2)n—OMs (n=3, 7, 11). For the chain elongation steps, 40-80% yields were achieved through extraction purification. PEG oligomer libraries I and II were generated in 50-95% overall yields by alkylation or acylation of THP-(OCH2CH2)n—OH (n=1-15) followed by deprotection. Alkylation of Me-(OCH2CH2)n—OH (n=1-11, 13) with X—(CH2)m—CO2R (X=Br or OMs) and subsequent hydrolysis led to PEG oligomer library III in 30-60% overall yields. Combinatorial purification techniques were adapted to the larger-scale library synthesis. A total of 498 compounds, each with a weight of 2-5 g and a minimum purity of 90%, were synthesized.
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Page/Page column 10
(2010/02/15)
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