Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
10596170 | Bioorganic & Medicinal Chemistry Letters | 2013 | 4 Pages |
Abstract
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.
Keywords
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
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,