A series of novel potent inhibitors of dipeptidyl peptidase IV (DPP-IV
) has been developed. A brief structure-activity relationship of the i
nhibitors was investigated. The dipeptide TSL-225, tophyl-1,2,3,4-tetr
ahydroisoquinoline-3-carboxylic acid, was identified with the critical
structure for the inhibitory activity. (C) 1998 Elsevier Science Ltd.
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