کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1362179 | 981480 | 2011 | 5 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Spirodiketopiperazine-based CCR5 antagonist: Discovery of an antiretroviral drug candidate
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موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
چکیده انگلیسی
Following the discovery that hydroxylated derivative 3 (Fig. 1) was one of the oxidative metabolites of the original lead 1, it was found that hydroxylated compound 4 possesses higher in vitro anti-HIV potency than the corresponding non-hydroxylated compound 2. Structural hybridation of 4 with the orally available analog 5 resulted in another orally-available spirodiketopiperazine CCR5 antagonist 6a that possesses more favorable pharmaceutical profile for use as a drug candidate.
Molecular design of a new orally-available CCR5 antagonist.Figure optionsDownload as PowerPoint slide
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 21, Issue 4, 15 February 2011, Pages 1141–1145
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 21, Issue 4, 15 February 2011, Pages 1141–1145
نویسندگان
Rena Nishizawa, Toshihiko Nishiyama, Katsuya Hisaichi, Chiaki Minamoto, Naoki Matsunaga, Yoshikazu Takaoka, Hisao Nakai, Stephen Jenkinson, Wieslaw M. Kazmierski, Hideaki Tada, Kenji Sagawa, Shiro Shibayama, Daikichi Fukushima, Kenji Maeda,