908258-58-2Relevant articles and documents
Synthesis of non-ionic bolaamphiphiles and study of their self-assembly and transport behaviour for drug delivery applications
Rashmi,Singh, Abhishek K.,Achazi, Katharina,Schade, Boris,B?ttcher, Christoph,Haag, Rainer,Sharma, Sunil K.
, p. 31777 - 31782 (2018/09/25)
A series of four bolaamphiphiles with different hydrophilic units has been synthesised. All the amphiphiles were well characterised from their physiochemical data. The aggregation tendency of newly synthesised amphiphiles was studied using fluorescence spectroscopy, dynamic light scattering (DLS), and cryogenic electron microscopy (cryo-TEM). Furthermore, their application as nanocarriers for hydrophobic guests was demonstrated by using two established standards, i.e. the dye Nile red and the drug nimodipine. A cytotoxicity and cellular uptake study has been carried out using A549 cells. Due to the presence of an ester linkage in PEG based bolaamphiphiles, a drug release study was performed in the presence of an immobilized enzyme Novozym-435 (a lipase).
Monodisperse oligoethylene glycols modified Propofol prodrugs
Deng, Tao,Mao, Xianglan,Li, Yu,Bo, Shaowei,Yang, Zhigang,Jiang, Zhong-Xing
, p. 3502 - 3505 (2018/10/15)
The low water solubility of Propofol resulted in complicated formulation and adverse effects during its clinical application. To improve its water solubility and maintain its anesthetic effects, Propofol prodrugs with monodisperse oligoethylene glycols as solubility enhancer were designed and synthesized. Monodisperse oligoethylene glycols enable the concise manipulation of water solubility, biocompatibility and anesthetic effects. Through the physicochemical and biological assay, a few water soluble prodrugs of Propofol were identified as promising anesthetic to overcome the drawbacks associated with Propofol.
Preparation and application of monodisperse polyethylene glycol monomethyl ether modified propofol prodrug
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Paragraph 0042; 0043; 0054; 0055, (2018/07/06)
Belonging to the field of organic chemistry and pharmaceutical chemicals, the invention discloses preparation and application of a monodisperse polyethylene glycol monomethyl ether modified propofol prodrug with a novel structure. Monodisperse polyethylene glycol monomethyl ether and propofol can be connected by an in-vivo degradable chemical bond to prepare a series of carbonic ester type and acetic ester type prodrugs respectively. By adjusting the length of the monodisperse polyethylene glycol monomethyl ether chain, the method can synthesize corresponding water-soluble propofol prodrugs, the longer the monodisperse polyethylene glycol monomethyl ether chain is, the better the water solubility is, along with the improvement of the water solubility, the prodrug can be made into aqueous solution preparations so as to avoid the defects of fat emulsion in propofol fat emulsions. The method provided by the invention has the advantages of simple reaction, mild conditions and low cost, andis convenient for industrial production.
Ceria supported gold-platinum catalysts for the selective oxidation of alkyl ethoxylates
Heidkamp, Katharina,Aytemir, Memet,Vorlop, Klaus-Dieter,Pruesse, Ulf
, p. 2984 - 2992 (2013/11/06)
This work covers the development of a ceria based AuPt catalyst for the selective aerobic oxidation of alkyl ethoxylates to their corresponding carboxylic acids. By optimizing metal loading and the Au to Pt ratio the activity of the catalyst could be increased significantly, while maintaining total selectivity. Although the choice of ceria as a support helped to suppress intermediate metal leaching, the catalyst still showed poor long-term stability in repeated batches. The cause for deactivation could finally be identified by TPR studies as over-oxidation. These suspicions were confirmed by a long-term stability study in continuous-mode. It proved to be possible to deactivate the catalyst on purpose by employing unfavourable oxidising reaction conditions, i.e. low substrate concentrations and excess oxygen. By avoiding such unfavourable conditions either in continuous-flow mode or in repeated batches, the long-term stability of the catalyst increased tremendously. A substrate screening of various ethoxylates showed that the catalyst was very well-suited to selectively oxidize a wide range of alkyl ethoxylates.
1-(2H)-ISOQUINOLONE DERIVATIVE
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Page/Page column 213, (2008/06/13)
The present invention provides a compound having high antitumor activity, which is useful for therapeutic and preventive agents effective for proliferative diseases such as cancer; a production method thereof; an intermediate compound useful for such production; and a pharmaceutical composition comprising such a compound. The present invention provides a compound represented by the formula (1): wherein X represents an aryl group or heteroaryl group which may be substituted, Cy represents a 4- to 7-membered monocyclic heterocyclic ring or a 8- to 10-membered condensed heterocyclic ring which may be substituted, and Z represents O, S, or NRa; or a prodrug thereof; or a pharmaceutically acceptable salt thereof; and a pharmaceutical and a pharmaceutical composition which comprise the compound.