Khan Khalid M, Saeed Sumayya, Ali Muhammad, Gohar Madiha, Zahid Javariya, Khan Ambreen, Perveen Shahnaz, Choudhary M Iqbal
HEJ Research Institute of Chemistry, International Center for Chemical and Biological Sciences, University of Karachi, Karachi 75270, Pakistan.
Bioorg Med Chem. 2009 Mar 15;17(6):2447-51. doi: 10.1016/j.bmc.2009.01.075. Epub 2009 Feb 9.
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.
已合成了一系列不对称二取代脲衍生物1 - 28，并对其体外抗糖化活性进行了筛选。化合物26（IC(50)=4.26±0.25微摩尔）、1（IC(50)=5.8±0.08微摩尔）、22（IC(50)=4.26±0.25微摩尔）、6（IC(50)=6.4±0.02微摩尔）、5（IC(50)=6.6±0.26微摩尔）、2（IC(50)=7.02±0.31微摩尔）、3（IC(50)=7.14±0.84微摩尔）、27（IC(50)=7.27±0.36微摩尔）、4（IC(50)=8.16±1.04微摩尔）、21（IC(50)=8.4±0.15微摩尔）、23（IC(50)=9.0±0.35微摩尔）和13（IC(50)=15.22±6.7微摩尔）表现出优异的抗糖化活性，远优于标准品（芦丁，IC(50)=41.9±2.3微摩尔）。因此，本研究为抗糖化剂的进一步研究提供了一系列潜在分子。
