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Synthesis, Structure–Activity Relationship and Docking Studies of Substituted Aryl Thiazolyl Phenylsulfonamides as Potential Protein Tyrosine Phosphatase 1B Inhibitors
Author(s) -
Varshney Kanika,
Gupta Swati,
Rahuja Neha,
Rawat Arun K.,
Singh Nagendra,
Tamarkar Akhilesh K.,
Srivastava Arvind K.,
Saxena Anil K.
Publication year - 2012
Publication title -
chemmedchem
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.817
H-Index - 100
eISSN - 1860-7187
pISSN - 1860-7179
DOI - 10.1002/cmdc.201200197
Subject(s) - docking (animal) , aryl , metformin , in vitro , protein tyrosine phosphatase , tyrosine , chemistry , phosphatase , computational biology , diabetes mellitus , biochemistry , pharmacology , stereochemistry , medicine , enzyme , biology , endocrinology , alkyl , nursing , organic chemistry
28 to 1—not bad odds: Protein tyrosine phosphatase 1B (PTP1B) is a promising target for the treatment of type 2 diabetes. Aryl thiazolyl phenylsulfonamides were synthesized and screened against PTP1B in vitro. Compounds exhibiting >48 % inhibition were then evaluated in a streptozotocin‐induced (STZ) rat model of diabetes, identifying one compound with efficacy comparable to that of metformin. Finally, docking studies were used to explain the observed structure–activity relationships.