کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1358132 | 981321 | 2016 | 18 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
1,2,4-Triazolyl octahydropyrrolo[2,3-b]pyrroles: A new series of potent and selective dopamine D3 receptor antagonists
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موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
چکیده انگلیسی
A novel series of 1,2,4-triazolyl octahydropyrrolo[2,3-b]pyrroles showing high affinity and selectivity at the DA D3 receptor is reported here. Compounds endowed with high selectivity over the hERG channel were identified and their pharmacokinetic properties thoroughly analyzed. A few derivatives with appropriate developability characteristics were selected for further studies and progression along the screening cascade. In particular, derivative 60a, (DA D3 pKi = 8.4, DA D2 pKi = 6.0 and hERG fpKi = 5.2) showed a balanced profile and further refinements are in progress around this molecule.
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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry - Volume 24, Issue 8, 15 April 2016, Pages 1619–1636
Journal: Bioorganic & Medicinal Chemistry - Volume 24, Issue 8, 15 April 2016, Pages 1619–1636
نویسندگان
Fabrizio Micheli, Andrea Bernardelli, Federica Bianchi, Simone Braggio, Laura Castelletti, Palmina Cavallini, Paolo Cavanni, Susanna Cremonesi, Michele Dal Cin, Aldo Feriani, Beatrice Oliosi, Teresa Semeraro, Luca Tarsi, Silvia Tomelleri, Andrea Wong,