Synthesis, biological evaluation and molecular modeling studies of arylidene-thiazolidinediones with potential hypoglycemic and hypolipidemic activities.
New arylidene-thiazolidinediones (ATZDs) were synthesized and evaluated in the alloxan-induced hyperglycemia mice model. The molecular target taken into consideration is the nuclear PPAR-gamma whose crystallographic structure is available on the PDB database as 2PRG. Thus the hypoglycemic and hypolipidemic activities of compounds were compared with the result of their docking after removal of the co-crystallized ligand present in the 2PRG structure. Molecular modeling studies were carried out using the Autodock 3.0.5 and ADT 1.1 programs.
da Costa Leite
Lúcia Fernanda C
LF
Departamento de Química, Universidade Católica de Pernambuco, Brazil.
Veras Mourão
Rosa Helena
RH
de Lima
Maria do Carmo Alves
Mdo C
Galdino
Suely Lins
SL
Hernandes
Marcelo Zaldini
MZ
de Assis Rocha Neves
Francisco
F
Vidal
Stéphanie
S
Barbe
Jacques
J
da Rocha Pitta
Ivan
I
D000496:Alloxan / Q000494:pharmacology; D000818:Animals; D001786:Blood Glucose / Q000378:metabolism; D003921:Diabetes Mellitus, Experimental / Q000139:chemically induced / Q000188:drug therapy; D004305:Dose-Response Relationship, Drug; D006860:Hydrogen Bonding; D007004:Hypoglycemic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000627:therapeutic use*; D000960:Hypolipidemic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000627:therapeutic use*; D008024:Ligands; D051379:Mice; D008958:Models, Molecular; D015394:Molecular Structure; D047493:PPAR alpha / Q000378:metabolism; D047495:PPAR gamma / Q000378:metabolism; D045162:Thiazolidinediones / Q000138:chemical synthesis* / Q000737:chemistry / Q000627:therapeutic use*; D014280:Triglycerides / Q000097:blood
D001786:Blood Glucose; D007004:Hypoglycemic Agents; D000960:Hypolipidemic Agents; D008024:Ligands; D047493:PPAR alpha; D047495:PPAR gamma; D045162:Thiazolidinediones; D014280:Triglycerides; D000496:Alloxan