Abstract

The unique electron deficiency and coordination property of boron led to a wide range of applications in chemistry, energy research, materials science and the life sciences. The use of boron-containing compounds as pharmaceutical agents has a long history, and recent developments have produced encouraging strides. Boron agents have been used for both radiotherapy and chemotherapy. In radiotherapy, boron neutron capture therapy (BNCT) has been investigated to treat various types of tumors, such as glioblastoma multiforme (GBM) of brain, head and neck tumors, etc. Boron agents playing essential roles in such treatments and other well-established areas have been discussed elsewhere. Organoboron compounds used to treat various diseases besides tumor treatments through BNCT technology have also marked an important milestone. Following the clinical introduction of bortezomib as an anti-cancer agent, benzoxaborole drugs, tavaborole and crisaborole, have been approved for clinical use in the treatments of onychomycosis and atopic dermatitis. Some heterocyclic organoboron compounds represent potentially promising candidates for anti-infective drugs. This review highlights the clinical applications and perspectives of organoboron compounds with the natural boron atoms in disease treatments without neutron irradiation. The main topic focuses on the therapeutic applications of organoboron compounds in the diseases of tuberculosis and antifungal activity, malaria, neglected tropical diseases and cryptosporidiosis and toxoplasmosis.

Highlights

  • (1) Tuberculosis is an infectious disease caused by Mycobacterium tuberculosis, which has a high level of mortality worldwide and has already gained resistance to first- and second-line therapy [1]. (2) Malaria is a disease caused by the Plasmodium parasite and accounts for one of the leading causes of death worldwide despite decades of strategic interventions aimed at reducing incidence and mortality [2]. (3) Neglected tropical diseases (NTDs) are a group of twenty highly parasitic, viral and bacterial diseases as classified by the World Health Organization (WHO) [2,3,4]

  • NTDs affect more than one billion people, especially children, and prevail in poor populations living in tropical and subtropical climates, causing a huge toll in terms of morbidity and mortality, as well as public economies [2,3,4], and (4) cryptosporidiosis and toxoplasmosis are other dangerous diseases caused by important protozoan pathogens of humans, while Cryptosporidium is a common cause of moderate-to-severe diarrhea in children under five years of age [5]

  • The negatively charged tetrahedral oxaborole group was placed at the phosphate position at the cleavage site and it interacted with the two catalytic zinc ions

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Summary

Introduction

Publisher’s Note: MDPI stays neutral with regard to jurisdictional claims in published maps and institutional affiliations. Many infectious diseases are caused by microorganisms, such as tuberculosis and malaria, and the current treatments for them are unsatisfactory as there are a few or no suitable drugs Four types of such frequently occurring diseases, in which organoboron compounds have already shown high potential as acceptable drug agents, have been selected to survey in this review. This review will focus on the particular type of bioactivity of organoboron compounds covering the medicinal applications in infectious disease caused by protozoa, fungi and helminths, describing progress in drug development, cytotoxicity and the proposed mechanisms of action. The review covers four areas of therapeutic applications of organoboron compounds: tuberculosis and antifungal activity, malaria, neglected tropical diseases and cryptosporidiosis and toxoplasmosis.

Tuberculosis
Benzoxaboroles
Structures
Peptidyl
A Formation
Malaria
Trypanosomiasis
Leishmaniasis
Cryptosporidiosis and Toxoplasmosis
Findings
Conclusions
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