کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1377741 | 981986 | 2006 | 5 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Arylpropionylpiperazines as antagonists of the human melanocortin-4 receptor
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موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
چکیده انگلیسی
A series of 3-arylpropionylpiperazines were synthesized as antagonists of the melanocortin-4 receptor. Their potency was found to be increased by replacing the α-methyl substituent of the initial lead 11 with a larger s-Bu or i-Bu group. Further potency enhancement was observed when a glycine or β-alanine was incorporated onto the benzylamine. Some compounds demonstrated good potency, moderate selectivity, and oral bioavailability.
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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 16, Issue 17, 1 September 2006, Pages 4674–4678
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 16, Issue 17, 1 September 2006, Pages 4674–4678
نویسندگان
Wanlong Jiang, Fabio C. Tucci, Caroline W. Chen, Melissa Arellano, Joe A. Tran, Nicole S. White, Dragan Marinkovic, Joseph Pontillo, Beth A. Fleck, Jenny Wen, John Saunders, Ajay Madan, Alan C. Foster, Chen Chen,