کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
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1356621 | 981138 | 2008 | 6 صفحه PDF | دانلود رایگان |
![عکس صفحه اول مقاله: The absolute configuration plays an important role in muscarinic activity of BGT-A and its analogs The absolute configuration plays an important role in muscarinic activity of BGT-A and its analogs](/preview/png/1356621.png)
Both enantiomers of 2, 3, and 4, three bioactive analogs of muscarinic agonist BGT-A were prepared respectively and underwent functional studies and radioreceptor binding assays. 6S enantiomers of 2, 3, and 4 showed obvious muscarinic activity, while 6R ones elicited little muscarinic activity by functional studies. Besides, the affinity of 6S enantiomers of 2, 3, and 4 was greatly larger than that of their 6R enantiomers respectively. All these pharmalogical results indicated the 6S configuration was beneficial for the active BGT-A analogs to bind with the muscarinic receptors. The finding was in good agreement with our previous SAR study to BGT-A and its active analogs by computational approach. The understanding to the relationship between muscarinic activity and absolute configuration will provide the basis for successive screening of BGT-A analogs as effective muscarinic agonists or antagonists in clinical use.
The results of functional studies and radioreceptor binding assays to both enantiomers of bioactive analogs of muscarinic agonist BGT-A indicated the 6S configuration was beneficial for the molecules to bind with the muscarinic receptors.Figure optionsDownload as PowerPoint slide
Journal: Bioorganic & Medicinal Chemistry - Volume 16, Issue 24, 15 December 2008, Pages 10251–10256