کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
10594290 | 981821 | 2012 | 5 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Synthesis of new opioid derivatives with a propellane skeleton and their pharmacologies: Part 3, novel propellane derivatives with pentacyclic skeletons
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موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
![عکس صفحه اول مقاله: Synthesis of new opioid derivatives with a propellane skeleton and their pharmacologies: Part 3, novel propellane derivatives with pentacyclic skeletons Synthesis of new opioid derivatives with a propellane skeleton and their pharmacologies: Part 3, novel propellane derivatives with pentacyclic skeletons](/preview/png/10594290.png)
چکیده انگلیسی
Previously reported propellane derivative KNT-42 preferred the κ receptor and functioned as a message part in the message-address concept, but its affinity for the κ receptor was not high. To improve affinity, we synthesized five pentacyclic propellane derivatives designed for the purpose of fixing the conformation of KNT-42. The etheno- and ethano-bridged derivatives SYK-347 and SYK-393 exhibited high affinity and selectivity for the κ receptor, whereas the other derivatives did not. These results would be due to the different ranges of movement of the basic nitrogens and less basicity of the nitrogens due to the electron withdrawing effect of the introduced hydroxy or keto group. SYK-347 and SYK-393 preferring the κ receptor were expected to be useful for designing selective ligands for opioid receptor types, especially the κ receptor.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 22, Issue 24, 15 December 2012, Pages 7697-7701
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 22, Issue 24, 15 December 2012, Pages 7697-7701
نویسندگان
Hideaki Fujii, Ryo Nakajima, Junko Akiyama, Naoshi Yamamoto, Shigeto Hirayama, Toru Nemoto, Hiroaki Gouda, Shuichi Hirono, Hiroshi Nagase,