4667-99-6Relevant articles and documents
Semisynthetic Antimycobacterial C-3 Silicate and C-3/C-21 Ester Derivatives of Fusidic Acid: Pharmacological Evaluation and Stability Studies in Liver Microsomes, Rat Plasma, and Mycobacterium tuberculosis culture
Njoroge, Mathew,Kaur, Gurminder,Espinoza-Moraga, Marlene,Wasuna, Antonina,Dziwornu, Godwin Akpeko,Seldon, Ronnett,Taylor, Dale,Okombo, John,Warner, Digby F.,Chibale, Kelly
, p. 1634 - 1644 (2019)
Fusidic acid (FA), a natural product fusidane triterpene-based antibiotic with unique structural features, is active in vitro against Mycobacterium tuberculosis, the causative agent of tuberculosis (TB). While possessing good pharmacokinetics in man, FA is rapidly metabolized in rodents, thus complicating proof-of-concept studies in this model. Toward the repositioning of FA as an anti-TB agent, we herein describe the synthesis, activity, and metabolism of FA and semisynthesized ester derivatives in rat liver microsomes, rat plasma, and mycobacterial cell culture. FA and derivative molecules with a free C-3 OH underwent species-specific metabolism to the corresponding 3-OH epimer, 3-epifusidic acid (3-epiFA). FA was also metabolized in rat plasma to form FA lactone. These additional routes of metabolism may contribute to the more rapid clearance of FA observed in rodents. C-3 alkyl and aryl esters functioned as classic prodrugs of FA, being hydrolyzed to FA in microsomes, plasma, and Mycobacterium tuberculosis culture. In contrast, C-3 silicate esters and C-21 esters were inert to hydrolysis and so did not act as prodrugs. The antimycobacterial activity of the C-3 silicate esters was comparable to that of FA, and these compounds were stable in microsomes and plasma, identifying them as potential candidates for evaluation in a rodent model of tuberculosis.
Synthesis of triethoxysilanol
Kazakova,Gorbatsevich,Skvortsova,Demchenko,Muzafarov
, p. 1350 - 1351 (2005)
Triethoxysilanol was isolated for the first time by hydrolysis of chloro(triethoxy)silane in an organic solvent in the presence of a heterogeneous base and identified as an individual compound. The synthesis of this compound made it possible to study its physicochemical properties and substantially extended its potentialities for the synthesis of hyperbranched polyethoxysiloxanes and functional oligomers.
Method for removing methyldichlorosilane and silicon tetrachloride impurities in trimethyl chlorosilane
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Paragraph 0037-0038; 0042-0044; 0049; 0051-0052; 0063; ..., (2021/08/25)
The invention relates to a method for removing methyldichlorosilane and silicon tetrachloride impurities in trimethyl chlorosilane, which comprises a hydrosilylation reaction, a partial esterification reaction and a complete esterification reaction. Firstly, a mixture of trimethylsilyl chloride containing methyldichlorosilane and silicon tetrachloride impurities is added to a reactor for hydrosilylation reaction, and the reaction product enters a separation system. The silicon tetrachloride in the mixture is partially esterified and reacted by adding the low-carbon alcohol as an esterifying agent, and the reaction product enters a separation system. Finally, the partially esterified product is further fully esterified to valuable tetraalkoxy silicon products. The high-efficiency recycling of trimethylchlorosilane is realized, and high-value utilization is also realized.
