The synthesis and biological evaluation of a series of amidinohydrazones (3a-h, 6a-c, 8 and 9) as potential nonsteroidal inhibitors of aldosterone synthase (CYP11B2) are described. The compounds were tested in vitro using CYP11B2-expressing fission yeast; they showed only marginal inhibitory effect. Compound 6c was evaluated for its effect on the formation of aldosterone, cortisol, androstenedione, and DHEA in the adrenocortical tumor cell line NCI-H295R. It exhibited no significant effect on the production of these products.