Therapeutic Potential of Boron-Containing Compounds

Abstract

Relative to carbon, hydrogen, nitrogen and oxygen, very little is currently known about boron in therapeutics. In addition, there are very few boron-containing natural products identified to date to serve as leads for medicinal chemists. Perceived risks of using boron and lack of synthetic methods to handle boron-containing compounds have caused the medicinal chemistry community to shy away from using the atom. However, physical, chemical and biological properties of boron offer medicinal chemists a rare opportunity to explore and pioneer new areas of drug discovery. Boron therapeutics are emerging that show different modes of inhibition against a variety of biological targets. With one boron-containing therapeutic agent on the market and several more in various stages of clinical trials, the occurrence of this class of compound is likely to grow over the next decade and boron could become widely accepted as a useful element in future drug discovery.

Evaluation of selected properties of a new root repair cement containing surface pre-reacted glass ionomer fillers

“…The ability of S-PRG cement to nearly eradicate P. gingivalis bacteria can be explained by considerable ion release with antibacterial activity such as boron, strontium, and fluoride. The antimicrobial ability of boron-containing compounds has been a subject of interest in recent years [31,32]. Indeed, boron-based antibacterial therapeutics were suggested to possess strong antibacterial activity against gram-negative infections due to their ability to inhibit various bacterial enzymes [33,34].…”

Current data regarding the structure-toxicity relationship of boron-containing compounds

“…Therefore, the increase in the number of studies on the biological activity of BCCs has led to an accumulation of knowledge in this field, as well as the successful synthesis and testing of some BCCs for medicinal purposes. This in turn has stimulated great interest among researchers to participate in this area of investigation, as well as a growing recognition by the pharmaceutical industry of the medicinal potential of BCCs (Kingma, 1958;Groziak, 2001;Baker, 2009;Das, 2013;Del Rosso, 2014;Soriano-Ursúa, 2014a).…”

Molecular recognition with boronic acids—applications in chemical biology

“…Although boric acid (B(OH) 3 ) is used in insecticides and herbicide, it has low toxicity in humans, with lethal doses comparable to that of sodium chloride, common table salt (B(OH) 3 : LD 50 =2660 mg/kg; NaCl: LD 50 =3,000 mg/kg) [7,78]. Deboronation can occur by a number of routes, the main ones being metal-catalysed hydrolytic cleavage [27,48] and oxidative deboronation carried out by enzymes including cytochrome P450 [40,44,59].…”