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Chem Pharm Bull (Tokyo)
; 53(10): 1314-7, 2005 Oct.
Article
in English
| MEDLINE
| ID: mdl-16204990
ABSTRACT
Herein we report the development of novel, potent and non-peptide luteinizing hormone releasing hormone (LHRH) antagonists. The optimization towards derivatives free from mechanism-based CYP3A4 inhibition is described. The identification of a main metabolite guided us towards structural modifications of the benzyl moiety, which resulted in significant improvements of the CYP3A4 profile, while maintaining potent LHRH antagonist activity.