Ic. Jacobson et al., STRUCTURE-BASED DESIGN AND SYNTHESIS OF A SERIES OF HYDROXAMIC ACIDS WITH A QUATERNARY-HYDROXY GROUP IN P1 AS INHIBITORS OF MATRIX METALLOPROTEINASES, Bioorganic & medicinal chemistry letters, 8(7), 1998, pp. 837-842
Examination of the S1 area of the active site of pro-stromelysin has l
ed us to the design of novel and potent inhibitors of matrix metallopr
oteinases containing constrained quaternary-hydroxy group at pi. The s
ynthesis and biological activity of these compounds with variations at
P1', P2', and P3' will be described. (C) 1998 The DuPont Merck Pharma
ceutical Company. Published by Elsevier Science Ltd. All rights reserv
ed.