HPLC of β-blockers enantiomers using chiral stationary phases

What is it about?

Beta-blockers or β-adrenergic antagonists are an important class of organic substances which are widely used to reduce the blood pressure of patients with corresponding cardiovascular diseases. It is known that only one enantiomer of beta blockers exhibits pharmaceutical activity, so only half of a racemic active pharmaceutical ingredient (API) is effective and the rest is considered inactive, but not an absolutely non-harmful component. So, it is important to know the enantiomeric purity of these drugs.

Featured Image

Why is it important?

Macrocyclic antibiotics represent a class of versatile chiral selectors for the separation of β-blockers enantiomers in HPLC. Eremomycin can be produced by using biochemical synthesis and contains many different chiral centers in its molecule. The most intriguing question is identification of those, which are responsible for the successfull separation of β-blockers enantiomers. At least, seven derivatives of eremomycin have been tested and it was found that the best enantioseparation of β-blockers was obtained for CSPs with eremosaminyl eremomycin aglycon and des-eremosamynyl eremomycin as chiral selectors. The structure fragments responsible for the chiral recognition of β-blockers enantiomers are identified. This knowledge will aloow to improve enantioselectivity of existing chiral selectors based on macrocyclic antibiotics.

Perspectives