67617-97-4Relevant articles and documents
Synthesis, SAR and docking studies of substituted aryl phenylthiazolyl phenylcarboxamide as potential protein tyrosine phosphatase 1B (PTP1B) inhibitors
Varshney, Kanika,Gupta, Amit K.,Rawat, Arun,Srivastava, Rohit,Mishra, Akansha,Saxena, Mridula,Srivastava, Arvind K.,Jain, Sudha,Saxena, Anil K.
, p. 1378 - 1389 (2019/06/24)
In our continued effort to discover novel PTP1B inhibitor with improved in vivo activity, we attempted to optimize our previously discovered lead compound by replacing the sulfonyl group with benzoyl group to yield compound II. Additional structural modif
Synthesis, Structure-Activity Relationship and Docking Studies of Substituted Aryl Thiazolyl Phenylsulfonamides as Potential Protein Tyrosine Phosphatase1B Inhibitors
Varshney, Kanika,Gupta, Swati,Rahuja, Neha,Rawat, Arun K.,Singh, Nagendra,Tamarkar, Akhilesh K.,Srivastava, Arvind K.,Saxena, Anil K.
scheme or table, p. 1185 - 1190 (2012/08/29)
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Synthesis and QSAR studies in 2-(N-aryl-N-aroyl)amino-4,5-dihydrothiazole derivatives as potential antithrombotic agents
Saxena, Anil K.,Pandey, Suresh K.,Seth,Singh,Dikshit,Carpy
, p. 2025 - 2034 (2007/10/03)
A series of 2-(N-aryl-N-aroyl)amino-4,5-dihydrothiazole derivatives have been synthesized via cyclocondensation of N-aryl thioureas with 2-bromoethylamine hydrobromide followed by the reaction of the product thus obtained with aroyl chlorides. Title compounds were evaluated for their antithrombotic activity in vivo in mice where one of these compound 29 provided 65% protection as compared to 77% protection offered by the standard Indomethacin. Quantitative Structure-Activity Relationship (QSAR) studies were performed on these compounds using physicochemical (hydrophobic, electronic, steric) parameter as independent and antithrombic activity as dependent parameter, where antithrombotic activity correlated best (r > 0.8) with electronic parameters (F, σ or μ) having high statistical significance > 99.9% (F2,22 > 15.0; F2,22α:0.001 = 11.0) suggesting that hydrophobic, steric and resonance factors are insignificant in this set of molecules for the activity.