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“Green” synthesis of bioactive compounds

Candida antarcticaEnzymatic synthesisLipase type BProdrug

Introduction

The invention relates to an enzymatic synthesis method of molecules with very poor solubility in water from which modified molecules are obtained as potential candidates for experimentation as new anti-inflammatory agents with greater solubility and therefore bioavailability.

Technical features

The purpose of the invention is to provide a “green” enzymatic synthesis method, alternative to the traditional chemical approach, which uses type B lipases coming from the microorganism Candida antarctica as a biocatalyst, in order to combine poorly soluble active ingredients with molecules of marked solubility in water. The molecule resulting from this synthesis takes the name of prodrug and will be more soluble than the starting active ingredient. The present innovation has made it possible to synthesize three new compounds obtained from the esterification of ibuprofen with erythritol, xylitol, sorbitol, with increased polarity and therefore solubility.

Possible Applications

  • The obtained compounds are potential candidates as new non-steroidal anti-inflammatory drugs for the treatment of pain up to musculoskeletal disorders such as osteoarthritis, and rheumatoid arthritis.
  • Production of highly pure pharmaceutical esters and in a selectively way

Advantages

  • Fine regulation of the reaction conditions (preliminary processes, choice of solvent, concentrations, temperatures, etc.)
  • Green approach that does not use toxic / carcerogenic chemicals and high temperatures
  • One-phase reaction system not dependent on the presence of water
  • Process that is highly flexible and can be extended to many varieties of compounds with acidic function and poor solubility