Benzothiazole benzimidazole (S)-isothiazolidinone derivatives as protein tyrosine phosphatase-1B inhibitors

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

“…These derivatives are potent, competitive, and reversible inhibitors of PTP1B. The substitution of the BTA and benzimidazole gave modest improvement in potency [248]. The BTA-indole-N-alkanoic acid synthesized for aldose reductase inhibitors.…”

Inhibition protein tyrosine phosphatases by an oxovanadium glutamate complex, Na2[VO(Glu)2(CH3OH)](Glu = glutamate)

“…PTP1B gene knockout or antisense studies in normal and diabetic mice have shown lowered blood glucose levels and improved insulin responsiveness through enhanced IR signaling in peripheral tissues (Elchebly et al 1999;Klaman et al 2000;Zinker et al 2002). Therefore, PTP1B inhibitors have been pursued to develop novel anti-diabetic drugs (Xie and Seto 2007;Na et al 2006;Alal et al 2006;Shrestha et al 2007;Sparks et al 2007;Maccari et al 2007;Winter et al 2005).…”

Chapter 6. Recent Advances in PTP1B Inhibitor Development for the Treatment of Type 2 Diabetes and Obesity

“…Incyte has published a series of molecules with the IZD group incorporated on various scaffolds, such as peptides, sulfonamides, and heterocycles. [107][108][109][110][111][112] Representative compounds from each class are summarized in Figure 6.7 (compounds 59-63). Their IC 50 values for PTP1B range from 10 to 180 nM, suggesting that IZD is an effective p-Tyr mimetic in inhibiting PTP1B.…”