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The synthesis and biological evaluation of 1-heteroarylmethyl 1,4-diazepane derivatives as potential T-type calcium channel blockers is described. In this study, we have identified the compound 211 exhibiting the most potent T-type calcium channel blocking activity with IC(50) value of 0.20 mu M, which is superior to that of mibefradil.

Synthesis and Biological Evaluation of 1-Heteroarylmethyl 1,4-Diazepanes Derivatives as Potential T-type Calcium Channel Blockers