کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1366074 | 981580 | 2007 | 4 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
α,α-Cyclic aminoacids as useful scaffolds for the preparation of hNK2 receptor antagonists
دانلود مقاله + سفارش ترجمه
دانلود مقاله ISI انگلیسی
رایگان برای ایرانیان
کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
چکیده انگلیسی
MEN 15596 is a small molecule, potent and selective antagonist of NK2 receptor, possessing high affinity and potency at the guinea-pig and human receptors whose pharmacological characterization has been recently published. Here we report how the corresponding class of compounds was derived from a tri-peptide library and the first optimization round to improve both in vitro activity and physicochemical properties.
In the search for a novel class of hNK2 antagonists, compound 1 was identified from a tripeptide library. Subsequent optimization of binding affinity and physicochemical properties afforded 43, subnanomolar hNK2 antagonist.Figure optionsDownload as PowerPoint slide
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 17, Issue 17, 1 September 2007, Pages 4841–4844
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 17, Issue 17, 1 September 2007, Pages 4841–4844
نویسندگان
Alessandro Sisto, Maria Altamura, Franco Cardinali, Piero D’Andrea, Cristina Rossi, Daniela Fattori,