کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1377330 | 981976 | 2008 | 5 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Potent heteroarylpiperidine and carboxyphenylpiperidine 1-alkyl-cyclopentane carboxamide CCR2 antagonists
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موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
![عکس صفحه اول مقاله: Potent heteroarylpiperidine and carboxyphenylpiperidine 1-alkyl-cyclopentane carboxamide CCR2 antagonists Potent heteroarylpiperidine and carboxyphenylpiperidine 1-alkyl-cyclopentane carboxamide CCR2 antagonists](/preview/png/1377330.png)
چکیده انگلیسی
This report describes replacement of the 4-(4-fluorophenyl)piperidine moiety in our CCR2 antagonists with 4-heteroaryl piperidine and 4-(carboxyphenyl)-piperidine subunits. Some of the resulting analogs retained potency in our CCR2 binding assay and had improved selectivity versus the IKr channel; poor selectivity against IKr had been a liability of earlier analogs in this series.
This report describes incorporation of 4-heteroaryl piperidine and 4-(carboxyphenyl)-piperidine subunits into our CCR2 antagonists, leading to new analogs retaining CCR2 potency, but with improved selectivity over IKr channel binding.Figure optionsDownload as PowerPoint slide
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 18, Issue 3, 1 February 2008, Pages 994–998
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 18, Issue 3, 1 February 2008, Pages 994–998
نویسندگان
Alexander Pasternak, Stephen D. Goble, Pasquale P. Vicario, Jerry Di Salvo, Julia M. Ayala, Mary Struthers, Julie A. DeMartino, Sander G. Mills, Lihu Yang,