Inhibitors of dopamine. beta.-hydroxylase. 3. Some 1-(pyridylmethyl) imidazole-2-thiones

…, EH Ohlstein, RW Erickson, M Ezekiel…

Index: Ross; Kruse; Ohlstein; Erickson; Ezekiel; Flaim; Sawyer; Berkowitz Journal of Medicinal Chemistry, 1987 , vol. 30, # 8 p. 1309 - 1313

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Citation Number: 24

Abstract

The 1-benzylimidazole-2-thione moiety has been previously shown by Kruse et al. to be broadly associated with dopamine@-hydroxylase (DBH) inhibitory activity both in vitro and in vivo in spontaneously hypertensive rats (SHR). An extension of structure-activity studies to 1-(pyridylmethy1)-and 1-(oxypyridylmethyl) imidazole-2-thiones is reported here in an attempt to exploit the pH differential that exists across the chromaffin vesicle membrane. ...