Synthesis, molecular docking and PTP1B inhibitory activity of functionalized 4,5-dihydronaphthofurans and dibenzofurans.
Protein tyrosine phosphatase 1B (PTP1B) is an enzyme that plays a critical role in down-regulating insulin signaling through dephosphorylation of the insulin receptor. Inhibitors of PTP1B showed increased insulin sensitivity and normalize plasma glucose level and thus are useful therapeutic agents for the treatment of diabetes. A series of functionalized 4,5-dihydronaphthofurans and dibenzofurans were synthesized, studied through molecular docking and evaluated for their PTP1B inhibitory activity.
Dixit
Manish
M
Division of Medicinal and Process Chemistry, Central Drug Research Institute, Lucknow 226001, India.
Saeed
Uzma
U
Kumar
Amit
A
Siddiqi
Mohammad Imran
MI
Tamrakar
Akhilesh K
AK
Srivastava
Arvind K
AK
Goel
Atul
A
D001572:Benzofurans / Q000138:chemical synthesis* / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology*; D001665:Binding Sites; D003198:Computer Simulation; D018360:Crystallography, X-Ray; D020128:Inhibitory Concentration 50; D007700:Kinetics; D008958:Models, Molecular; D008968:Molecular Conformation; D009281:Naphthalenes / Q000138:chemical synthesis* / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology*; D017027:Protein Tyrosine Phosphatases / Q000037:antagonists & inhibitors* / Q000378:metabolism*
D001572:Benzofurans; D009281:Naphthalenes; C023614:dibenzofuran; D017027:Protein Tyrosine Phosphatases