Unsymmetrically disubstituted urea derivatives: a potent class of antiglycating agents

Khalid M Khan; Sumayya Saeed; Muhammad Ali; Madiha Gohar; Javariya Zahid; Ambreen Khan; Shahnaz Perveen; M Iqbal Choudhary

doi:10.1016/j.bmc.2009.01.075

Unsymmetrically disubstituted urea derivatives: a potent class of antiglycating agents

Bioorg Med Chem. 2009 Mar 15;17(6):2447-51. doi: 10.1016/j.bmc.2009.01.075. Epub 2009 Feb 9.

Authors

Khalid M Khan¹, Sumayya Saeed, Muhammad Ali, Madiha Gohar, Javariya Zahid, Ambreen Khan, Shahnaz Perveen, M Iqbal Choudhary

Affiliation

¹ HEJ Research Institute of Chemistry, International Center for Chemical and Biological Sciences, University of Karachi, Karachi 75270, Pakistan. [email protected]

PMID: 19251423
DOI: 10.1016/j.bmc.2009.01.075

Abstract

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.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Glucose / antagonists & inhibitors*
Glucose / chemistry
Magnetic Resonance Spectroscopy
Spectrometry, Mass, Electrospray Ionization
Urea / analogs & derivatives*
Urea / pharmacology*

Substances

Urea
Glucose