Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
10587111 | Bioorganic & Medicinal Chemistry Letters | 2014 | 4 Pages |
Abstract
A design for the selective release of drug molecules in the liver was tested, involving the attachment of a representative active agent by an ester linkage to various 2-substituted 5-aminovaleric acid carbamates. The anticipated pathway of carboxylesterase-1-mediated carbamate cleavage followed by lactamization and drug release was frustrated by unexpectedly high sensitivity of the ester linkage toward hydrolysis by carboxylesterase-2 and other microsomal components.
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Authors
Srinivas R. Chirapu, Jonathan N. Bauman, Heather Eng, Theunis C. Goosen, Timothy J. Strelevitz, Subhash C. Sinha, Robert L. Dow, M.G. Finn,