کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1374053 | 981912 | 2012 | 5 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Structure–activity relationships and molecular modeling of the N-(3-pivaloyloxy-2-benzylpropyl)-N′-[4-(methylsulfonylamino)benzyl] thiourea template for TRPV1 antagonism
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
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چکیده انگلیسی
The structure–activity relationships of N-(3-acyloxy-2-benzylpropyl)-N′-4-[(methylsulfonylamino)benzyl] thioureas, which represent simplified RTX-based vanilloids, were investigated by varying the distances between the four principal pharmacophores and assessing binding and antagonistic activity on rTRPV1. The analysis indicated that a 3-pivaloyloxy-2-benzylpropyl C-region conferred the best potency in binding affinity and antagonism. The molecular modeling of this best template with the tetrameric homology model of rTRPV1 was performed to identify its binding interactions with the receptor.
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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 22, Issue 11, 1 June 2012, Pages 3656–3660
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 22, Issue 11, 1 June 2012, Pages 3656–3660
نویسندگان
Rahul S. Bhondwe, Dong Wook Kang, Myeong Seop Kim, Ho Shin Kim, Seul-gi Park, Karam Son, Sun Choi, Krystle A. Lang Kuhs, Vladimir A. Pavlyukovets, Larry V. Pearce, Peter M. Blumberg, Jeewoo Lee,