Synthesis of protein tyrosine phosphatase 1B inhibitors: model validation and docking studies.
The designed and synthesized 2-(4-methoxyphenyl) ethyl] acetamide derivatives (3a, 3b and 3c) were evaluated for their PTP1B inhibitory activity where they showed IC(50) values 69 microM, 87 microM and 71 microM, respectively. These results correlated well with the docking studies and in vivo screening of the compounds for their antidiabetic activity in SLM and STZ models.
Saxena
Anil K
AK
Central Drug Research Institute, Medicinal and Process Chemistry, Chattar Manzil Palace, Mahatma Gandhi Marg, Lucknow, Uttar Pradesh, India. anilsak@gmail.com
Pandey
Gyanendra
G
Gupta
Swati
S
Singh
Amar Bahadur
AB
Srivastava
Arvind K
AK
D000818:Animals; D001665:Binding Sites / Q000502:physiology; D018360:Crystallography, X-Ray; D003921:Diabetes Mellitus, Experimental / Q000188:drug therapy* / Q000201:enzymology; D016503:Drug Delivery Systems / Q000379:methods*; D007004:Hypoglycemic Agents / Q000138:chemical synthesis* / Q000378:metabolism / Q000627:therapeutic use; D008958:Models, Molecular; D054562:Protein Tyrosine Phosphatase, Non-Receptor Type 1 / Q000037:antagonists & inhibitors* / Q000737:chemistry* / Q000378:metabolism; D051381:Rats
D007004:Hypoglycemic Agents; D054562:Protein Tyrosine Phosphatase, Non-Receptor Type 1