Vardhan Doddahindaiah M Suyoga, Shantharam Chavalmane S, Suhas Ramesh, Sridhara Malavalli B, Gowda D Channe
Department of Studies in Chemistry, University of Mysore, Manasagangotri, Mysore--570 006, Karnataka, India.
Protein Pept Lett. 2013 Aug;20(8):888-97. doi: 10.2174/0929866511320080005.
Synthesis of a series of urea and thiourea derivatives of glycine and proline conjugated to 2,3-dichlorophenyl piperazine has been reported. The structures were confirmed by physical and spectroscopical measurements followed by characterization of antiglycation activity. All synthesized compounds were able to inhibit protein glycation, particularly halogen containing derivatives without preference of oxygen or sulphur at the urea function. The best analogues are nearly 20 fold (< 5 µM) more potent than the reference standard, rutin (41.9 µM).
据报道，已合成了一系列与2,3-二氯苯基哌嗪共轭的甘氨酸和脯氨酸的脲和硫脲衍生物。通过物理和光谱测量确定其结构，随后对其抗糖化活性进行表征。所有合成化合物均能抑制蛋白质糖化，特别是含卤素的衍生物，在脲官能团处对氧或硫无偏好。最佳类似物的效力比参考标准芦丁（41.9 µM）高近20倍（<5 µM）。
