BROMINATION-A VERSATILE TOOL FOR DRUGS OPTIMIZATION
BROMINATION-A VERSATILE TOOL FOR DRUGS OPTIMIZATION (Abstract): Scientific literature presents many naturally occurring brominated substances exhibiting different biological activities. Most natural brominated derivatives have been isolated from the marine biosphere, being metabolites of algae, sponges and corals. These molecules became structural models for obtaining synthetic derivatives with superior bioactive potential. The present paper is an analysis of previously published studies on the influence of insertion of bromine atoms in different molecules on their bioactivity. In general, the results confirmed the positive effect of bromination on the bioactive potential of substances. The mechanisms explaining these results are still insufficiently elucidated, several possibilities being mentioned: increased lipophilicity and permeability through biological membranes, increased half-life or the possibility of intermolecular bond formation (attractive interactions) between the electrophilic region of the molecule containing bromine atoms and various nucleophilic active sites of biomolecules. In conclusion, bromination may be a way to increase the potency of therapeutic agents and research in the field of molecular design of brominated compounds will certainly continue.
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