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Amino-alcohol dipeptide analogues: A simple synthesis of a versatile isostere for the development of proteinase inhibitors

✍ Scribed by R.J. Arrowsmith; D.E Davies; Y.C. Fogden; C.J. Harris; C. Thompson

Publisher: Elsevier Science
Year: 1987
Tongue: French
Weight: 155 KB
Volume: 28
Category: Article
ISSN: 0040-4039
DOI: 10.1016/s0040-4039(00)96784-4

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✦ Synopsis

Two sample approaches to an ammo-alcohol isostere of proteolytrcally-cleavable dipeptrde sequences are descrrbed; this isostere is incorporated into stereochemically-defined tetrapeptlde analogues. We1 and others2 have shown that replacement of the cleavable amrde bond of appropriate peptide substrates by a novel ammo-alcohol rsostere (-v'-(CH(OH)CHZ)-), (1) IS a versatile approach to potent

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