Unsymmetrically disubstituted urea derivatives: a potent class of antiglycating agents.
A series of unsymmetrically disubstituted urea derivatives 1-28 has been synthesized and screened for their antiglycation activity in vitro. Compounds 26 (IC(50)=4.26+/-0.25 microM), 1 (IC(50)=5.8+/-0.08 microM), 22 (IC(50)=4.26+/-0.25 microM), 6 (IC(50)=6.4+/-0.02 microM), 5 (IC(50)=6.6+/-0.26 microM), 2 (IC(50)=7.02+/-0.31 microM), 3 (IC(50)=7.14+/-0.84 microM), 27 (IC(50)=7.27+/-0.36 microM), 4 (IC(50)=8.16+/-1.04 microM), 21 (IC(50)=8.4+/-0.15 microM), 23 (IC(50)=9.0+/-0.35 microM) and 13 (IC(50)=15.22+/-6.7 microM) showed an excellent antiglycation activity far better than the standard (rutin, IC(50)=41.9+/-2.3 microM). This study thus provides a series of potential molecules for further studies of antiglycation agents.
Khan
Khalid M
KM
HEJ Research Institute of Chemistry, International Center for Chemical and Biological Sciences, University of Karachi, Karachi 75270, Pakistan. khalid.khan@iccs.edu
Saeed
Sumayya
S
Ali
Muhammad
M
Gohar
Madiha
M
Zahid
Javariya
J
Khan
Ambreen
A
Perveen
Shahnaz
S
Choudhary
M Iqbal
MI
D005947:Glucose / Q000037:antagonists & inhibitors* / Q000737:chemistry; D009682:Magnetic Resonance Spectroscopy; D021241:Spectrometry, Mass, Electrospray Ionization; D014508:Urea / Q000031:analogs & derivatives* / Q000494:pharmacology*
D014508:Urea; D005947:Glucose