Bioactive boron compounds inspired from Nature

Boron can be primarily found in a wide variety of natural sources such as fruits, vegetables, and hazelnuts. It is an essential nutrient useful or necessary for the development of organisms. It plays a significant role in plantsʼ structural integrity and metabolism, whereas in mammals it is essential for bone health and proper function of vitamin D [1]. Furthermore, boron exists in natural antibiotics, such as Boromycin, Asplasmomycin, Borophycin, and Tartrolons, possessing antibacterial, anticancer, and antiviral properties [2].

A variety of boron-containing bioactive compounds exhibit antibacterial, antifungal, antiparasitic, antiviral and anti-inflammatory activities [3]; some of these compounds have been recently approved by FDA as commercially available drugs. Velcade^® and Ninlaro^® are proteasome inhibitors for the treatment of multiple myeloma. Kerydin^® is a benzoxaborole to treat fungal onychomycosis. Eucrisa^® combats mild to moderate atopic dermatitis. Vabomere^® is a combination drug, including Vaborbactam (a boronic acid component), a β-lactamase inhibitor, and Meropenem which impedes the synthesis of bacterial cell-wall, thus treating bacterial infections [1]. Calcium fructoborate (CFB) is a nature-identical mimetic of a molecule naturally present in fruits and is commercially produced as a dietary boron supplement for combating inflammatory and cardiovascular diseases and killing cancer cells [2].

Based on the above and our interest in boron derivatives, we designed the synthesis of bioactive boron-containing heterocycles and proceeded to the evaluation of their antioxidant and anti-inflammatory properties with the aim to develop new drug entities [4].

The authors are grateful to Alan and Linde Katritzky Foundation, ARKAT USA, for financial support of the research.

Fig. 1 Boron-containing heterocycles.

Publication History

Article published online:
12 December 2022

• References

• 1 Ji L, Zhou H. Recent developments in the synthesis of bioactive boron-containing compounds. Tetrahedron Lett 2021; 82: 153411
• 2 Dembitsky VM, Gloriozova TA. Naturally Occurring Boron Containing Compounds and Their Biological Activities. J Nat Prod Resour 2017; 3: 147-154
• 3 Diaz DB, Yudin AK. The versatility of boron in biological target engagement. Nat Chem 2017; 9: 731-742
• 4 Kotali A, Maniadaki A, Kotali E. et al. New tetrahedral boron heterobicycles: Cyclocondensation of phenylboronic acid with β-keto butanoic acid N-acyl hydrazones. Tetrahedron Lett 2017; 58: 512-515 and references therein