Heterocycle-substituted 1,5-benzothiazepines: biological properties and structure–activity relationships

Abstract

1,5-Benzothiazepines represent key scaffolds in medicinal chemistry because of their applicability in a wide variety of pharmaceuticals. Many cardiovascular, antidepressant, and antipsychotic drugs on the market accommodate this privileged structure, but the biological effects of 1,5-benzothiazepines are much more diverse, including enzyme inhibitory, antimicrobial, central nervous system depressant, anti-inflammatory, and anticancer activity. The introduction of a heterocyclic substituent onto a chemical structure can be beneficial in terms of bioactivity and drug-like properties. In this review, the biological activities of 1,5-benzothiazepines with and without heterocyclic substituents are discussed and compared. In some cases, the addition of a heterocycle proved to be beneficial for enhancing activity, especially the introduction of a 2-thienyl group, and also the position of heteroatoms in the substituent can have an impact on the overall properties of the resulting compounds.

Graphical abstract