کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1377398 | 981977 | 2007 | 4 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Synthesis and SAR of tetrahydropyrrolo[1,2-b][1,2,5]thiadiazol-2(3H)-one 1,1-dioxide analogues as highly potent selective androgen receptor modulators
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
![عکس صفحه اول مقاله: Synthesis and SAR of tetrahydropyrrolo[1,2-b][1,2,5]thiadiazol-2(3H)-one 1,1-dioxide analogues as highly potent selective androgen receptor modulators Synthesis and SAR of tetrahydropyrrolo[1,2-b][1,2,5]thiadiazol-2(3H)-one 1,1-dioxide analogues as highly potent selective androgen receptor modulators](/preview/png/1377398.png)
چکیده انگلیسی
Replacement of the 3-oxo group of 2-chloro-4-[(7R,7aS)-7-hydroxy-1,3-dioxotetrahydro-1H-pyrrolo[1,2c]imidazol-2(3H)-yl]-3-methylbenzonitrile resulted in a sulfamide series of selective androgen receptor modulator (SARM) agonists.
Herein, we report the effects of replacing the 3-oxo group of 2 with a sulfonyl group (e.g., 3). These tetrahydropyrrolo[1,2-b][1,2,5]thiadiazol-2(3H)-one 1,1-dioxide analogues were found to be potent SARMs. Synthesis, binding and functional assay SAR, as well as in vivo characterization of a selected analogue in a standard rodent model are presented.Figure optionsDownload as PowerPoint slide
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 17, Issue 16, 15 August 2007, Pages 4487–4490
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 17, Issue 16, 15 August 2007, Pages 4487–4490
نویسندگان
Mark C. Manfredi, Yingzhi Bi, Alexandra A. Nirschl, James C. Sutton, Ramakrishna Seethala, Rajasree Golla, Blake C. Beehler, Paul G. Sleph, Gary J. Grover, Jacek Ostrowski, Lawrence G. Hamann,