By Justus Scout
Boronic acids and their derivatives are used in medicinal chemistry and organic synthesis because of their versatility in preparing complex molecules. Boronic acids are also used in various reactions. These include electrophilic allyl shifts, homologations, conjugate additions, lieberskind-srogl coupling, chan-lam coupling, sonogashira coupling, Stille coupling, and more.
In addition, boronic acids are used in biological applications, such as inhibition of serine proteases. For more information about boronic acids and derivatives, read on:
Application of Boronic Acids
Boronic acid is usually a stable and non-toxic group easy to synthesize. These features make boric acids useful in synthetic reactions. They include acid catalysis, hydroboration, and asymmetric synthesis of amino acids.
They are also used in drugs, but as aryl boronic acids form. Heterocycles with boronic acids such as pyrrolyl, indolyl, and pyridinyl derivatives are used in medicinal chemistry.
Here are the biological uses of boronic acids:
Anticancer Activity
Cellular homeostasis results from the deterioration of intracellular proteins. It is possible because of essential ubiquitin-proteasome pathway action. The pathway helps regulate apoptosis and the cell cycle by stabilizing proteins like a tumor suppressor. Therefore, it makes proteasome a target for cancer therapy.
The boronic acid group is used to help increase the potency of this proteasome inhibitor. It is also used because of its high selectivity rates towards the proteasome. When present, it causes disruption of the complex protein and inhibits the growth of apoptosis of cancer cells.
Antibacterial Activity
Antibiotic resistance is a significant concern in human health. Therefore, bacteria resistance will be associated with various classes due to Gram-negative bacteria. The best thing, boronic acid can act as reactive power. It can connect with the serine residue of the enzyme to act as an inhibitor.
The characteristics of boric acids show they are essential in forming novel compounds to act as an antibiotic.
Antiviral Activity
Boronic acids can combine with carbohydrates and thus, allowing for the treatment of viruses. Some of these viruses are those with high glycosylated envelops like the human immunodeficiency virus.
Moreover, their physicochemical characteristics show they are associated with the biological application.
Sensors and Delivery Systems
Most of the uses mentioned above of boronic acids derivatives depend on their specific roles as enzyme inhibitors. However, other boronic acids derivatives are used in drug delivery systems and sensors. This is from their ability to react reversibly, thus acting as sensors of carbohydrates. So, helpful in monitoring some diseases such as diabetes.
Other Boron-Containing Compounds
Boronic acids aren’t the only compounds with boron elements; other compounds have interesting and therapeutic applications. Some of these compounds include boron esters, benzoxaboroles, and diazaborines.
Diazaborines used to be the first compound with boron investigated to have therapeutic properties. They were identified to be antimicrobial agents. They showed to have similarities with antibiotic nitrofurantoin. The compounds are effective against Gram-negative bacteria.
Conclusion
If you handling chemical compounds, you must be careful. Some are hazardous and may cause health problems and death. There are always precaution measures from the manufacturer to follow. Following the guidance ensures safety!
