Benzimidazole-5-sulfonamides as novel nonpeptide luteinizing hormone releasing hormone (LHRH) antagonists: minimization of mechanism-based CYP3A4 inhibition.

@article{Hashimoto2005Benzimidazole5sulfonamidesAN,
  title={Benzimidazole-5-sulfonamides as novel nonpeptide luteinizing hormone releasing hormone (LHRH) antagonists: minimization of mechanism-based CYP3A4 inhibition.},
  author={Kentaro Hashimoto and Mikayo Kataoka and Miyuki Tatsuta and Kayo Yasoshima and Mako Yamamoto and Takeshi Yura and Noriyuki Yamamoto and Klaus Urbahns and Jang Bahadur Gupta and Yingfu Li},
  journal={Chemical & pharmaceutical bulletin},
  year={2005},
  volume={53 10},
  pages={1314-7}
}
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. 

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