Synthesis, in vitro and computational studies of protein tyrosine phosphatase 1B inhibition of a small library of 2-arylsulfonylaminobenzothiazoles with antihyperglycemic activity

A comprehensive review in current developments of benzothiazole-based molecules in medicinal chemistry

“…Compounds 212(a,b) have exhibited most promising activity as mixed-type inhibitors of PTP-1D. These compounds also show antihyperglycemic activity in a type 2 diabetes mellitus rat model, they lowering plasma glucose concentration, during the 7 h postintragastric administration [246]. Benzothiazol-2-oxoacetate derivatives exhibited good protein tyrosine phosphatase 1B inhibitory activity in the low micro-molar range.…”

“…Cathepsin K (Cat K) is highly expressed in osteoclasts and plays a key role in bone resorption by the degradation of type I cartilage. BTA derivatives (246) found this potent inhibitor of Cat K had good dog PK and the margin to hERG ion channel inhibition was deemed too low for a clinical candidate [280]. BTA-thiazoleimidazole conjugated compounds were synthesized and evaluated for ALK5 inhibitors in an enzyme assay and for their TGF-binduced Smad2/3 phosphorylation inhibitory activity in a cellbased assay.…”

Benzothiazoles: How Relevant in Cancer Drug Design Strategy?

“…Benzothiazole (Fig. 1), a heterocyclic compound constitutes an important scaffold of drugs, which can serve as unique and versatile ligand for experimental drug design [8] and have attracted attention because of their varied biological activities that pertain to antitumor [9], antitubercular [10], antimalarial [11], anticonvulsant [12], antidiabetic [13], antimicrobial, antihelmintic [14], analgesic, antiinflammatory [15], diuretic [16] etc. Some of the bis-benzothiazole derivatives exhibit their importance in amyloid-imaging [17], as vulcanization accelerators and also as starting materials for the synthesis of various drugs.…”

Synthesis, Structure–Activity Relationship and Docking Studies of Substituted Aryl Thiazolyl Phenylsulfonamides as Potential Protein Tyrosine Phosphatase 1B Inhibitors

“…[5] Efforts are being made to discover orally active and selective PTP1B inhibitors that could be useful for probing signal transduction pathways as well as for the treatment of diabetes and obesity. [21] Most of the inhibitors containing multiple charged phosphate mimicking components cannot be developed into effective drugs because of their low cell permeability and bioavailability. [21] Most of the inhibitors containing multiple charged phosphate mimicking components cannot be developed into effective drugs because of their low cell permeability and bioavailability.…”