کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
7771538 | 1500437 | 2018 | 11 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Design, synthesis and biological evaluation of bitopic arylpiperazine-hexahydro-pyrazinoquinolines as preferential dopamine D3 receptor ligands
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موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
چکیده انگلیسی
Three series of bitobic arylpiperazine-phenyl-hexahydropyrazinoquino- lines analogues were designed, synthesizedand evaluated as a novel class of selective ligands for the dopamine D3 receptor. Compounds 15a (Ki of 11.7â¯Â±â¯1.8 and 373â¯nM at D3 and D2, respectively), 15c (Ki of 5.49 and 264â¯nM at D3 and D2, respectively), 15e (Ki of 14.9 and 325â¯nM at D3 and D2, respectively), 15i (Ki of 13.8 and 401â¯nM at D3 and D2, respectively) and 15l (Ki of 13.6 and 870â¯nM at D3 and D2, respectively) were found to demonstrate good binding affinity and selectivity, and especially compound 15c showeda similar binding affinity and selectivity compared with the contrast drug BP897.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic Chemistry - Volume 77, April 2018, Pages 125-135
Journal: Bioorganic Chemistry - Volume 77, April 2018, Pages 125-135
نویسندگان
Benhua Zhou, Min Ji, Jin Cai,