Diamine Derivatives Containing Imidazolidinylidene Propanedinitrile as a New Class of Histamine H3 Receptor Antagonists: Conformationally Restricted Derivatives

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  • Sasho Setsuya
    Medicinal Chemistry Research Laboratories, Pharmaceutical Research Center, Kyowa Hakko Kogyo Co., Ltd.
  • Seishi Takashi
    Medicinal Chemistry Research Laboratories, Pharmaceutical Research Center, Kyowa Hakko Kogyo Co., Ltd.
  • Kawamura Mariko
    Medicinal Chemistry Research Laboratories, Pharmaceutical Research Center, Kyowa Hakko Kogyo Co., Ltd.
  • Tomuro Misato
    Medicinal Chemistry Research Laboratories, Pharmaceutical Research Center, Kyowa Hakko Kogyo Co., Ltd.
  • Hirose Ryo
    Medicinal Chemistry Research Laboratories, Pharmaceutical Research Center, Kyowa Hakko Kogyo Co., Ltd.
  • Toki Shinichiro
    Medicinal Chemistry Research Laboratories, Pharmaceutical Research Center, Kyowa Hakko Kogyo Co., Ltd.
  • Shimada Junich
    Medicinal Chemistry Research Laboratories, Pharmaceutical Research Center, Kyowa Hakko Kogyo Co., Ltd.

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Abstract

Novel conformationally restricted diamine derivatives containing imidazolidinylidene propanedinitrile were synthesized and evaluated for human and rat histamine H3 receptor (H3R) binding affinities. Among them, compounds 2b, 2c, 2j, 2k and 2m were found to be potent ligands for both H3Rs with Ki values in the sub-nanomolar range, and showed potent H3 receptor antagonism.

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