TY  - JOUR
PY  - 2002//
TI  - 1-Alkoxycarbonyl-3-halogenoazetidin-2-ones as elastase (PPE) inhibitors
JO  - Bioorganic and medicinal chemistry
A1  - Gérard, Stéphane
A1  - Nollet, Gaëtan
A1  - Vande Put, Jennifer
A1  - Marchand-Brynaert, Jacqueline
SP  - 3955
EP  - 3964
VL  - 10
IS  - 12
N2  - A series of 1-alkoxycarbonyl-3-halogenoazetidin-2-ones, designed as potential suicide inhibitors of serine proteases, has been synthesized and evaluated against porcine pancreatic elastase (PPE). All the compounds were transient inhibitors, their activity depending mainly on the nature of the halogen substituent: bromo- and iodo- derivatives are more active (K(i) approximately 2-22 microM) than 3-chloroazetidinones (K(i) approximately 20-150 microM). The lipophilicity of the N-1 substituent appeared to exert a slightly positive effect.<p /> <p>Language: en</p>
LA  - en
SN  - 0968-0896
UR  - http://dx.doi.org/10.1016/s0968-0896(02)00304-8
ID  - ref1
ER  -