Novel 1,4-benzothiazine derivatives as large conductance Ca2+-activated potassium channel openers.

Abstract

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).

DOI: 10.1021/jm701605f

Cite this paper

@article{Calderone2008Novel1D, title={Novel 1,4-benzothiazine derivatives as large conductance Ca2+-activated potassium channel openers.}, author={Vincenzo Calderone and Roberto Spogli and Alma Martelli and Giuseppe Manfroni and Lara Testai and Stefano Sabatini and Oriana Tabarrini and Violetta Cecchetti}, journal={Journal of medicinal chemistry}, year={2008}, volume={51 16}, pages={5085-92} }