Benzimidazole-5-sulfonamides as novel nonpeptide luteinizing hormone releasing hormone (LHRH) antagonists: minimization of mechanism-based CYP3A4 inhibition |
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| Authors: | Hashimoto Kentaro Kataoka Mikayo Tatsuta Miyuki Yasoshima Kayo Yamamoto Mako Yura Takeshi Yamamoto Noriyuki Urbahns Klaus Gupta Jang Bahadur Li Yingfu |
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| Institution: | Research Center Kyoto, Bayer Yakuhin, Ltd., Kyoto, Japan. kentaro.hashimoto@bayerhealthcare.com |
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| 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. |
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