Journal
ORGANIC LETTERS
Volume 4, Issue 4, Pages 549-552Publisher
AMER CHEMICAL SOC
DOI: 10.1021/ol010282n
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- NHLBI NIH HHS [HL-59931] Funding Source: Medline
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The objective of this work was to synthesize cyclic prodrugs 1a and 1b from Aggrastat 2a and its analogue 2b, respectively, to improve their membrane permeation. Cyclic prodrugs is and 1b were formed using an ester bond between the -COON group of Aggrastat or its analogue and the phenylpropionic acid linker 3 and an amide bond between the piperidinylamine and the -COOH group of the linker 3, respectively, as outlined in Scheme 4.
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