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6. Solid-phase synthesis of a combinatorial array of 1,3-bis(acylamino)-2-butanones, inhibitors of the cysteine proteases cathepsins K and L.

Author

Yamashita DS, Dong X, Oh HJ, Brook CS, Tomaszek TA, Szewczuk L, Tew DG, and Veber DF

Subjects
Butanones chemistry, Butanones pharmacology, Cathepsin K, Cathepsin L, Cysteine Endopeptidases, Cysteine Proteinase Inhibitors chemistry, Cysteine Proteinase Inhibitors pharmacology, Drug Design, Kinetics, Models, Molecular, Structure-Activity Relationship, Butanones chemical synthesis, Cathepsins antagonists & inhibitors, Combinatorial Chemistry Techniques methods, Cysteine Proteinase Inhibitors chemical synthesis, Endopeptidases
Abstract

To more rapidly prepare members of the 1,3-bis(acylamino)-2-butanone class of cysteine protease inhibitors, a solid-phase synthesis was developed. 1-Azido-3-amino-2,2-dimethoxybutane (4), which has the two amino groups differentiated and the ketone protected as a a ketal, served as a surrogate for the 1,3-diamino-2-butanone core. Amine (4) was coupled to the BAL-resin-linked carboxylic acids derived from alpha-amino acid esters. Evaluation of a small combinatorial array by measuring inhibition constants (Ki,appS) against cathepsins K, L, and B provided some structure-activity relationship trends with respect to selectivity and potency. Novel, potent inhibitors of cathepsins K and L were identified.

Published
1999
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