Title of article
Benzimidazole derivatives as novel nonpeptide luteinizing hormone-releasing hormone (LHRH) antagonists. Part 2: Benzimidazole-5-sulfonamides
Author/Authors
Yingfu Li، نويسنده , , Mikayo Kataoka، نويسنده , , Miyuki Tatsuta، نويسنده , , Kayo Yasoshima، نويسنده , , Takeshi Yura، نويسنده , , Klaus Urbahns، نويسنده , , Atsushi Kiba، نويسنده , , Noriyuki Yamamoto ، نويسنده , , Jang B. Gupta، نويسنده , , Kentaro Hashimoto، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2005
Pages
3
From page
805
To page
807
Abstract
The 2-cyclopropyl substituted benzimidazole 2 has been used as a starting point for further optimization of an LHRH antagonist series. SAR studies revealed that a tert-butyl urea fragment connected through a simple carbon chain would improve activity. Further modification of the benzylsulfonamide moiety led to the discovery of 23 (IC50: 4.2 nM).
Keywords
LHRH antagonist , Small molecule
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2005
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
795291
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