کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1378191 | 981996 | 2005 | 5 صفحه PDF | دانلود رایگان |
Linear pentapeptides (Penta-cis-Apc-DPhe-Arg-Trp-Gly-NH2) containing 1-amino-4-phenylcyclohexane-1-carboxylic acid (cis-Apc) and substituted Apc are potent hMC4R agonists and they are inactive or weakly active in hMC1R, hMC3R, and hMC5R agonist assays. This study, together with our earlier report on 5-BrAtc, demonstrated the importance of replacing His6 with phenyl-containing rigid templates in achieving good hMC4R agonist potency and selectivity against hMC1R in linear pentapeptides.
A design and synthesis of cis-Apc as new histidine surrogate and its incorporation into linear pentapeptides (Penta-cis-Apc-DPhe-Arg-Trp-Gly-NH2) and related analogs leading to potent and selective hMC4R agonists are reported.Figure optionsDownload as PowerPoint slide
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 15, Issue 22, 15 November 2005, Pages 4910–4914