کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
10596170 | 981897 | 2013 | 4 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Inhibitors of HIV-1 attachment. Part 9: An assessment of oral prodrug approaches to improve the plasma exposure of a tetrazole-containing derivative
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
![عکس صفحه اول مقاله: Inhibitors of HIV-1 attachment. Part 9: An assessment of oral prodrug approaches to improve the plasma exposure of a tetrazole-containing derivative Inhibitors of HIV-1 attachment. Part 9: An assessment of oral prodrug approaches to improve the plasma exposure of a tetrazole-containing derivative](/preview/png/10596170.png)
چکیده انگلیسی
N-Acetoxymethyl 4, N-pivaloyloxymethyl 5, and N-methyl 6 were evaluated as potential oral prodrugs of the parent tetrazole 3 in rats. Prodrug 5 was ineffective in improving the plasma concentration of 3 in vivo but compound 4 provided a 15-fold enhancement of the plasma concentration of 3. Most interestingly, oral dosing of analog 6 afforded a substantial increase in the plasma concentration of 3 in rats when compared to dosing of 3. This represents a novel example of a methyl tetrazole that acts as a prodrug for a free NH tetrazole-containing compound.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 23, Issue 1, 1 January 2013, Pages 209-212
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 23, Issue 1, 1 January 2013, Pages 209-212
نویسندگان
Kap-Sun Yeung, Zhilei Qiu, Zheng Yang, Lisa Zadjura, Celia J. D'Arienzo, Marc R. Browning, Steven Hansel, Xiaohua Stella Huang, Betsy J. Eggers, Keith Riccardi, Ping-Fang Lin, Nicholas A. Meanwell, John F. Kadow,