کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1363656 | 981519 | 2008 | 24 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
2-Phenyl-4-piperazinylbenzimidazoles: Orally active inhibitors of the gonadotropin releasing hormone (GnRH) receptor
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
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چکیده انگلیسی
Antagonism of the gonadotropin releasing hormone (GnRH) receptor has shown positive clinical results in numerous reproductive tissue disorders such as endometriosis, prostate cancer and others. Traditional therapy has been limited to peptide agonists and antagonists. Recently, small molecule GnRH antagonists have emerged as potentially new treatments. This article describes the discovery of 2-phenyl-4-piperazinylbenzimidazoles as small molecule GnRH antagonists with nanomolar potency in in vitro binding and functional assays, excellent bioavailability (rat %F > 70) and demonstrated oral activity in a rat model having shown significant serum leuteinizing hormone (LH) suppression.
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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry - Volume 16, Issue 13, 1 July 2008, Pages 6617–6640
Journal: Bioorganic & Medicinal Chemistry - Volume 16, Issue 13, 1 July 2008, Pages 6617–6640
نویسندگان
Jeffrey C. Pelletier, Murty Chengalvala, Josh Cottom, Irene Feingold, Lloyd Garrick, Daniel Green, Diane Hauze, Christine Huselton, James Jetter, Wenling Kao, Gregory S. Kopf, Joseph T. Lundquist IV, Charles Mann, John Mehlmann, John Rogers,