ENANTIOMERS, METABOLISM AND STRUCTURE-ACTIVITY RELATIONSHIPS OF 3-BENZAZEPINE DERIVATIVES

Mutlu Dilsiz AYTEMIR*, Dilek Demir EROL*°

*Hacettepe University, Faculty of Pharmacy, Department of Pharmaceutical Chemistry, Sihhiye-Ankara, TURKEY.
°Corresponding Author

Summary:
This study covers the interaction of many 3-benzazepine derivatives with Dopamine (DA) receptors. The tetrahydro-3-benzazepine ring system is of interest from a medicinal chemistry viewpoint since it incorporates the phenethylamine skeleton , which is so common in nature and in many drugs in a unique and moderately constrained way. The benzazepines share this feature with the isoquinoline family compounds. Relatively few
3-benzazepine alkoloids have been identified and prior to 1960 few investigations of the potential therapeutic utility of 3-benzazepine derivatives accessible by synthesis had been reported. Since that time, research directed to the synthesis and biological evaluation of the 3-benzazepines has been carried out in the laboratories of pharmaceutical industry. Several
3-benzazepines currently under study are likely candidates for clinical evaluation . Much of the research in this area has focused on the chemistry of compounds which interact more or less selectively with dopamine (DA) receptor systems in the periphery and/or the central nervous system. The purpose of this article is to review the literature since 1968 and to provide the reader with a current overview of the enantiomers, metabolism and structure-activity relationship of 3-benzazepine derivatives.

Key words:
Benzazepine, Enantiomer, Adenylate Cyclase Stimulation, Renal Vasodilator.