کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1366155 981582 2006 16 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Synthesis of 3,6-diazabicyclo[3.1.1]heptanes as novel ligands for the opioid receptors
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Synthesis of 3,6-diazabicyclo[3.1.1]heptanes as novel ligands for the opioid receptors
چکیده انگلیسی

In an effort to improve diazabicycloalkane-based opioid receptor ligands, N-3(6)-arylpropenyl-N-6(3)-propionyl-3,6-diazabicyclo[3.1.1]heptanes (3A,Ba–i) were synthesized and their affinity and selectivity towards μ-, δ- and κ-receptors were evaluated.The results of the current study revealed a number of compounds (3Bb, 3Bg and 3Bh) having a high affinity for μ (Ki at μ-receptors ranging from 2.7 to 7.9 nM) versus δ (Ki at δ-receptors >2000 nM) and versus κ (Ki at κ-receptors >5000 nM) receptors.Molecular modelling carried out on the pair 3Aa/3Ba and on the 3Bh was consistent with the hypothesis that the two series of compounds 3A and 3B interact with the μ-receptor in very different ways.

Figure optionsDownload as PowerPoint slide

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry - Volume 14, Issue 3, 1 February 2006, Pages 676–691
نویسندگان
, , , , , , , , ,