کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1358768 | 981361 | 2012 | 9 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
2-(4-Methylsulfonylaminophenyl) propanamide TRPV1 antagonists: Structure–activity relationships in the B and C-regions
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
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چکیده انگلیسی
On the basis of the previous lead N-4-t-butylbenzyl 2-(3-fluoro-4-methylsulfonylaminophenyl) propanamide (3) as a potent TRPV1 antagonist, structure–activity relationships for the B (propanamide part) and C-region (4-t-butylbenzyl part) have been investigated for rTRPV1 in CHO cells. The B-region was modified with dimethyl, cyclopropyl and reverse amides and then the C-region was replaced with 4-substituted phenyl, aryl alkyl and diaryl alkyl derivatives. Among them, compound 50 showed high binding affinity with Ki = 21.5 nM, which was twofold more potent than 3 and compound 54 exhibited potent antagonism with Ki(ant) = 8.0 nM comparable to 3.
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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry - Volume 20, Issue 3, 1 February 2012, Pages 1310–1318
Journal: Bioorganic & Medicinal Chemistry - Volume 20, Issue 3, 1 February 2012, Pages 1310–1318
نویسندگان
Wei Sun, Keliang Liu, HyungChul Ryu, Dong Wook Kang, Yong Soo Kim, Myeong Seop Kim, Yongsung Cho, Rahul S. Bhondwe, Shivaji A. Thorat, Ho Shin Kim, Larry V. Pearce, Vladimir A. Pavlyukovets, Richard Tran, Matthew A. Morgan, Jozsef Lazar,