Journal
EXPERT OPINION ON THERAPEUTIC PATENTS
Volume 28, Issue 6, Pages 493-504Publisher
TAYLOR & FRANCIS LTD
DOI: 10.1080/13543776.2018.1473379
Keywords
Benzoxaborole; anti-bacterial agents; anti-fungal agents; anti-protozoal agents; anti-viral agents; anti-inflammatory agents; enzyme inhibitors
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Introduction: Benzoxaborole is a versatile boron-heterocyclic scaffold which has found in the last 10 years a broad spectrum of applications in medicinal chemistry, due to its physicochemical and drug-like properties. Use of benzoxaborole moiety in the design of compounds led to the discovery of new classes of anti-bacterial, anti-fungal, anti-protozoal, anti-viral as well as anti-inflammatory agents with interesting drug development perspectives. Areas covered: This article reviews the patent literature as well as chemistry literature during the period 2010-2018 where in several benzoxaborole derivatives with therapeutic options were reported. Expert opinion: Two benzoxaborole derivatives are already clinically used for the treatment of onychomycosis (tavaborole) and atopic dermatitis (crisaborole), with several others in various phases of clinical trials. By inhibiting enzymes essential in the life cycle of fungal, protozoan, bacterial and viral pathogens, it is probable that other compounds may soon enter the armamentarium of anti-infective agents. On the other hand, phosphodiesterase 4 seems to be the human target responsible of the anti-inflammatory action of some benzoxaboroles. The chemical versatility, peculiar mechanism of action related to the electron deficient nature of the boron atom, and ease of preparation make benzoxaboroles a highly interesting field for the pharmaceutical industry.
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