Design Synthesis and Bioevaluation of Novel Bile Acid Conjugate

Abstract

newline This thesis briefly introduces bile acid conjugates and their therapeutic applications. Nature continues to be the main source of motivation for synthetic chemists in their expedition to prepare novel conjugates, which can have different physical, biological and medicinal properties. newlineChapter 1 describes the literature report available on bile acid and bile acid-based conjugates with their therapeutic importance in the development of drug. In recent years, steroid structures have gradually become important in various fields, such as pharmacology, bio-mimetic and supramolecular chemistry, and nanotechnology. The administration of bile acids has received a lot of attention. The drug absorption enhancer ability of bile acid helps to dissolve the drug and penetrate the drug molecule. Therefore, bile acids can increase the bioavailability of drugs with poor water solubility or poor membrane permeability. In addition, the hydroxyl and carboxyl functional groups of bile acids can be used for covalent bonding of biologically active molecules, thereby changing the physicochemical and pharmacokinetic properties of biologically active molecules. Syntheses of hybrid molecules via the combination of two bioactive moieties have appeared as a successful strategy in the development of novel therapeutic agents with excellent potency and lower side effects. With this in mind and fetching an advantage from the prevailing bile acid-based conjugates, we planned to synthesize bile acid-chiral amino alcohols/chalcones/thiadiazoles conjugate. newline newlineChapter 2 describes the synthesis, characterization and antibacterial evaluation of deoxycholic acid-chiral amino alcohol conjugates. Various amino alcohols moieties were appended to the C24 position of deoxycholic acid to yield deoxycholic acid-amino alcohol conjugates. The entire synthesized deoxycholic acid-amino alcohol conjugates were evaluated for their antibacterial activity against . coli and S. aureus using the broth dilution method.