Small molecule antagonists of the gonadotropin-releasing hormone (GnRH) receptor: Structure–activity relationships of small heterocyclic groups appended to the 2-phenyl-4-piperazinyl-benzimidazole template

Diane B. Hauze,Murty V. Chengalvala,Joshua E. Cottom,Irene B. Feingold,Lloyd Garrick,Daniel M. Green,Christine Huselton,Wenling Kao,Kenneth Kees,Joseph T. Lundquist,Charles W. Mann,John F. Mehlmann,John F. Rogers,Linda Shanno,Jay Wrobel,Jeffrey C. Pelletier

Bioorganic & Medicinal Chemistry Letters（2009）

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摘要

The potent GnRH antagonist template, 2-(4-tert-butylphenyl)-4-(1-piperazinyl)benzimidazole was appended to several small heterocycles. The N-ethylimidazole 32 was screened for in vivo pharmacokinetic and GnRH activity in rats.

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关键词

Gonadotropin releasing hormone (GnRH) receptor,2-Phenyl-4-piperazinyl-benzimidazole

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