Synthesis of Amidinohydrazones and Evaluation of Their Inhibitory Effect towards Aldosterone Synthase (CYP11B2) and the Formation of Selected Steroids

Abstract
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.

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