کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
9769266 | 1501247 | 2005 | 19 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Anthranilic acid based CCK1 receptor antagonists: preliminary investigation on their second “touch point”
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
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چکیده انگلیسی
In this phase of structure-affinity relationship study of VL-0395, a new anthranilic acid based CCK1 selective antagonist, we propose a series of unnatural aminoacidic derivatives. The result of this work is the identification of a new CCK ligand, which possesses an affinity (IC50 = 35 nm) one order of magnitude greater than the lead and, as a general rule, it points out how the hypothesized receptorial pocket which accommodates the Phe residue allows much more structural modification than that interacting with the N-terminal group. Hence, the modification of the C-terminal pharmacophoric group of our lead VL-0395 can not only enhance the affinity of anthranilic acid derivatives but can modulate the selectivity for one CCK receptor subtype or afford mixed antagonists.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: European Journal of Medicinal Chemistry - Volume 40, Issue 6, June 2005, Pages 563-581
Journal: European Journal of Medicinal Chemistry - Volume 40, Issue 6, June 2005, Pages 563-581
نویسندگان
Antonio Varnavas, Lucia Lassiani, Valentina Valenta, Laura Mennuni, Francesco Makovec, Dimitra Hadjipavlou-Litina,