کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
10582577 | 981052 | 2013 | 13 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Australian marine sponge alkaloids as a new class of glycine-gated chloride channel receptor modulator
ترجمه فارسی عنوان
آلکالوئیدهای اسفنج دریایی استرالیا به عنوان یک کلاس جدید از مولکول گیرنده کانال کلرید گلیسین
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موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
چکیده انگلیسی
Chemical analysis of a specimen of the sponge Ianthella cf. flabelliformis returned two new sesquiterpene glycinyl lactams, ianthellalactams A (1) and B (2), the known sponge sesquiterpene dictyodendrillin (3) and its ethanolysis artifact ethyl dictyodendrillin (4), and five known sponge indole alkaloids, aplysinopsin (5), 8E-3â²-deimino-3â²-oxoaplysinopsin (6), 8Z-3â²-deimino-3â²-oxoaplysinopsin (7), dihydroaplysinopsin (8) and tubastrindole B (9). The equilibrated mixture 6/7 exhibited glycine-gated chloride channel receptor (GlyR) antagonist activity with a bias towards α3 over α1 GlyR, while tubastrindole B (9) exhibited a bias towards α1 over α3 GlyR. At low- to sub-micromolar concentrations, 9 was also a selective potentiator of α1 GlyR, with no effect on α3 GlyR-a pharmacology that could prove useful in the treatment of movement disorders such as spasticity and hyperekplexia. Our investigations into the GlyR modulatory properties of 1-9 were further supported by the synthesis of a number of structurally related indole alkaloids.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry - Volume 21, Issue 14, 15 July 2013, Pages 4420-4425
Journal: Bioorganic & Medicinal Chemistry - Volume 21, Issue 14, 15 July 2013, Pages 4420-4425
نویسندگان
Walter Balansa, Robiul Islam, Daniel F. Gilbert, Frank Fontaine, Xue Xiao, Hua Zhang, Andrew M. Piggott, Joseph W. Lynch, Robert J. Capon,