Novel 1,4-benzothiazine derivatives show promise as large-conductance calcium-activated potassium channel openers with potent vasorelaxant activity in vitro.
These derivatives merit further preclinical evaluation as BK openers; leaves open clinical translation for vasorelaxant therapy.
The design and synthesis of a novel class of 1,4-benzothiazines targeted for the large-conductance calcium-activated potassium channels (BK) are presented. In vitro functional characterization of BK channel opening activity was assessed by measuring the relaxation of isolated rat aortic rings precontracted with KCl 20 mM. The results of this study show that the 1,4-benzothiazine heterocyclic nucleus is a suitable backbone for designing novel BK-openers; indeed, some of these new 1,4-benzothiazine derivatives had a vasorelaxant potency comparable or superior to that of reference BK-activator NS-1619 (1).
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Calderone et al. (2008) studied this question.
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