Introducing bromine in the molecular structure as a good strategy to the drug design

Eduard Potapskyi; Karolina Kustrzyńska; Dawid Łażewski; Paulina Skupin-Mrugalska; Roman Lesyk; Marcin Wierzchowski

doi:10.20883/medical.e1128

Authors

Eduard Potapskyi Chair and Department of Chemical Technology of Drugs, Poznan University of Medical Sciences, Poland https://orcid.org/0000-0002-5248-1091
Karolina Kustrzyńska Department of Inorganic and Analytical Chemistry, Poznan University of Medical Sciences, Poland https://orcid.org/0009-0004-1108-4569
Dawid Łażewski Chair and Department of Chemical Technology of Drugs, Poznan University of Medical Sciences, Poland https://orcid.org/0000-0002-9832-5094
Paulina Skupin-Mrugalska Department of Inorganic and Analytical Chemistry, Poznan University of Medical Sciences, Poland https://orcid.org/0000-0002-2495-6504
Roman Lesyk Department of Pharmaceutical, Organic and Bioorganic Chemistry, Danylo Halytsky Lviv National Medical University, Lviv, Ukraine https://orcid.org/0000-0002-3322-0080
Marcin Wierzchowski Chair and Department of Chemical Technology of Drugs, Poznan University of Medical Sciences, Poland https://orcid.org/0000-0003-2619-0466

DOI:

https://doi.org/10.20883/medical.e1128

Keywords:

bromine, halogen bond, radiopharmacy, drug resistance

Abstract

Nowadays, the search for new pharmaceuticals results in the development of thousands of new substances. One of the effective drug design strategies is to modify a previously obtained and studied substance. A very popular modification is the introduction of halogens into the structure of drugs, most often these are fluorine or chlorine atoms. However, the introduction of bromine into the structure of a potential drug also has a number of advantages. A good example would be natural substances extracted from marine organisms, which have been studied and proven to be effective in various diseases, including antibiotic therapy of resistant bacteria. Numerous studies justify the usage of bromine and its isotopes in therapy (both in diagnostic imaging and radiotherapy). To better explain the impact of “bromination,” numerous researchers have described such a phenomenon as “halogen bond.” Due to the presence of the so-called “sigma-hole” in the halogen atom of an organic molecule, it is possible to form these bonds, which results in a change in intermolecular and intramolecular interactions. Such changes can favorably affect drug-target interactions. The advantages of “bromination” include an increase in therapeutic activity, a beneficial effect on the metabolism of the drug and an increase in its duration of action. Besides, the phenomenon of heavy atom effect can be used to increase the effectiveness of photodynamic therapy and radiosensitization. Unfortunately, “bromination” is not without drawbacks, which we may include increased toxic effects and accumulation in the organism.

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