Bicyclic cyanothiazolidines as novel dipeptidyl peptidase 4 inhibitors.

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Betancort JM, Winn DT, Liu R, Xu Q, Liu J, Liao W, Chen SH, Carney D, Hanway D, Schmeits J, Li X, Gordon E, Campbell DA

Bicyclic cyanothiazolidines as novel dipeptidyl peptidase 4 inhibitors.

Bioorg Med Chem Lett. 2009 Aug 1;19(15):4437-40. doi: 10.1016/j.bmcl.2009.05.048. Epub 2009 May 18.

PubMed ID

19482472 [ View in PubMed

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Abstract

The synthesis and biochemical evaluation of novel cyanothiazolidine inhibitors of dipeptidyl peptidase 4 (DPP4) is described. Their main structural feature is a constrained bicyclic core that prevents the intramolecular formation of inactive cyclic species. The inhibitors show good to moderate biochemical potency against DPP4 and display distinct selectivity profiles towards DPP7, DPP8 and DPP9 depending on their substitution.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Saxagliptin	Dipeptidyl peptidase 4	IC 50 (nM)	3	N/A	N/A	Details
Vildagliptin	Dipeptidyl peptidase 4	IC 50 (nM)	3	N/A	N/A	Details