کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
10587087 | 981416 | 2014 | 4 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
IV. Discovery of CXCR3 antagonists substituted with heterocycles as amide surrogates: Improved PK, hERG and metabolic profiles
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موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
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چکیده انگلیسی
The structure-human CXCR3 binding affinity relationship of a series of pyridyl/pyrazinyl-piperazinyl-piperidine derivatives were explored with a focus to improve PK, hERG and metabolic profiles. Several small heterocycles were identified as amide surrogates, which minimized many potential metabolite issues. During the course of SAR development, we have observed the additive effect of desirable functional groups to improve hERG and PK profiles which lead to the discovery of many clinically developable CXCR3 antagonists with excellent overall profile.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 24, Issue 4, 15 February 2014, Pages 1085-1088
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 24, Issue 4, 15 February 2014, Pages 1085-1088
نویسندگان
Anilkumar G. Nair, Michael K.C. Wong, Youheng Shu, Yueheng Jiang, Chung-Her Jenh, Seong Heon Kim, De-Yi Yang, Qingbei Zeng, Yuefei Shao, Lisa Guise Zawacki, Jingqi Duo, Brian F. McGuinness, Carolyn DiIanni Carroll, Doug W. Hobbs, Neng-Yang Shih,