Synthesis of Amidinohydrazones and Evaluation of Their Inhibitory Effect towards Aldosterone Synthase (CYP11B2) and the Formation of Selected Steroids
- 29 June 2004
- journal article
- research article
- Published by Wiley in Archiv der Pharmazie
- Vol. 337 (7) , 411-416
- https://doi.org/10.1002/ardp.200400872
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.Keywords
This publication has 13 references indexed in Scilit:
- Development of a test system for inhibitors of human aldosterone synthase (CYP11B2): screening in fission yeast and evaluation of selectivity in V79 cellsThe Journal of Steroid Biochemistry and Molecular Biology, 2002
- Induction of Cardiac Fibrosis by AldosteroneJournal of Molecular and Cellular Cardiology, 2000
- The Effect of Spironolactone on Morbidity and Mortality in Patients with Severe Heart FailureNew England Journal of Medicine, 1999
- Steroidal and Nonsteroidal Sulfamates as Potent Inhibitors of Steroid SulfataseJournal of Medicinal Chemistry, 1998
- Further Definition of the D1 Dopamine Receptor Pharmacophore: Synthesis of trans-6,6a,7,8,9,13b-Hexahydro-5H-benzo[d]naphth[2,1-b]azepines as Rigid Analogues of β-PhenyldopamineJournal of Medicinal Chemistry, 1997
- Discovery and Optimization of a Novel Class of Orally Active Nonpeptidic Endothelin-A Receptor AntagonistsJournal of Medicinal Chemistry, 1996
- Guanabenz-related amidinohydrazones: potent non-azole inhibitors of aldosterone biosynthesisEuropean Journal of Medicinal Chemistry, 1994
- The NCI-H295 cell line: a pluripotent model for human adrenocortical studiesMolecular and Cellular Endocrinology, 1994
- Role of steroid 11 beta-hydroxylase and steroid 18-hydroxylase in the biosynthesis of glucocorticoids and mineralocorticoids in humans.Proceedings of the National Academy of Sciences, 1992
- Potential antisecretory antidiarrheals. 1. .alpha.2-Adrenergic aromatic aminoguanidine hydrazonesJournal of Medicinal Chemistry, 1988