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Synthesis and characterization of drug–saccharide conjugates by enzymatic strategy in organic media

Paper ID Volume ID Publish Year Pages File Format Full-Text
18084 42711 2007 8 PDF Available
Title
Synthesis and characterization of drug–saccharide conjugates by enzymatic strategy in organic media
Abstract

A facile and efficient strategy to prepare drug derivatives with saccharides was developed, and 12 drug–saccharide conjugates were obtained by selective enzymatic synthesis methods. When the transesterification of chlorphenesin vinyl esters with glucose was chosen as a model reaction, the influence of reaction conditions was optimized. Then, we successfully prepared a series of chlorphenesin–saccharide derivatives of three monosaccharides (glucose, mannose and galactose) and three disaccharides (maltose, lactose and sucrose). In order to study the relationship between the solubility of drug–saccharide conjugates and the structure of parent drugs, five hydrophobic drugs (chlorphenesin, mephenesin, guaifenesin, propranolol and clorprenaline) were chosen as substrates to synthesize drug–saccharide conjugates. The results indicated that the aqueous solublity of drug–saccharide derivatives was greatly improved, which was changed by different saccharides and the structure of parent drugs.

Keywords
Drug–saccharide conjugates; Solubility; Enzymatic synthesis; Organic media
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Synthesis and characterization of drug–saccharide conjugates by enzymatic strategy in organic media
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Publisher
Database: Elsevier - ScienceDirect
Journal: Enzyme and Microbial Technology - Volume 41, Issues 6–7, 1 November 2007, Pages 756–763
Authors
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Subjects
Physical Sciences and Engineering Chemical Engineering Bioengineering
Get Full-Text Now
Don't Miss Today's Special Offer
Price was $35.95
You save - $31
Price after discount Only $4.95
100% Money Back Guarantee
Full-text PDF Download
Online Support
Any Questions? feel free to contact us