TY - JOUR
T1 - Structure-Activity relationship of human serum Paraoxonase PON1
AU - Bargota, Rakesh
AU - Akhtar, Mahmoud
AU - Biggadike, K
AU - Gani, David
AU - Allemann, Rudolf
PY - 2003/5/19
Y1 - 2003/5/19
N2 - Substrate analogues based on the parent compounds paraoxon and phenyl acetate were tested on human serum paraoxonase (PON1) to explore the active site of the enzyme. Replacement of the nitro group of paraoxon with an amine or hydrogen, as well as electronic changes to the parent compound, converted these analogues into inhibitors. Introduction of either electron-withdrawing or donating groups onto phenyl acetate resulted in reduction in their rate of hydrolysis by PON1.
AB - Substrate analogues based on the parent compounds paraoxon and phenyl acetate were tested on human serum paraoxonase (PON1) to explore the active site of the enzyme. Replacement of the nitro group of paraoxon with an amine or hydrogen, as well as electronic changes to the parent compound, converted these analogues into inhibitors. Introduction of either electron-withdrawing or donating groups onto phenyl acetate resulted in reduction in their rate of hydrolysis by PON1.
UR - http://www.scopus.com/inward/record.url?scp=0037687922&partnerID=8YFLogxK
U2 - 10.1016/S0960-894X(03)00290-7
DO - 10.1016/S0960-894X(03)00290-7
M3 - Article
C2 - 12729627
VL - 13
SP - 1623
EP - 1626
JO - Bioorganic & Medicinal Chemistry Letters
JF - Bioorganic & Medicinal Chemistry Letters
IS - 10
ER -