title: Synthesis and SAR studies of urea and thiourea derivatives of gly/pro conjugated to piperazine analogue as potential AGE inhibitors.
abstract: 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).
authors: Department of Studies in Chemistry, University of Mysore, Manasagangotri, Mysore--570 006, Karnataka, India.
authors: Doddahindaiah M Suyoga
authors: DM
authors: Vardhan
authors: Chavalmane S
authors: CS
authors: Shantharam
authors: Ramesh
authors: R
authors: Suhas
authors: Malavalli B
authors: MB
authors: Sridhara
authors: D Channe
authors: DC
authors: Gowda
mesh_terms: D017127:Glycation End Products, Advanced / Q000037:antagonists & inhibitors*; D005998:Glycine / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D006801:Humans; D015394:Molecular Structure; D010671:Phenylurea Compounds / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D010879:Piperazines / Q000737:chemistry / Q000494:pharmacology; D011392:Proline / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D013329:Structure-Activity Relationship; D013890:Thiourea / Q000031:analogs & derivatives / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology
chemical_list: D017127:Glycation End Products, Advanced; D010671:Phenylurea Compounds; D010879:Piperazines; D011392:Proline; D013890:Thiourea; D005998:Glycine