Structure-based design and synthesis of benzimidazole derivatives as dipeptidyl peptidase IV inhibitors.

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Wallace MB, Feng J, Zhang Z, Skene RJ, Shi L, Caster CL, Kassel DB, Xu R, Gwaltney SL 2nd

Structure-based design and synthesis of benzimidazole derivatives as dipeptidyl peptidase IV inhibitors.

Bioorg Med Chem Lett. 2008 Apr 1;18(7):2362-7. doi: 10.1016/j.bmcl.2008.02.071. Epub 2008 Mar 4.

PubMed ID

18346892 [ View in PubMed

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Abstract

A novel series of non-covalent, benzimidazole-based inhibitors of DPP-4 has been developed from a small fragment hit using structure-based drug design. A highly versatile synthetic route was created for the development of SAR, which led to the discovery of potent and selective inhibitors with excellent pharmaceutical properties.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
1-biphenyl-2-ylmethanamine	Dipeptidyl peptidase 4	IC 50 (nM)	30000	N/A	N/A	Details
7-(aminomethyl)-6-(2-chlorophenyl)-1-methyl-1H-benzimidazole-5-carbonitrile	Dipeptidyl peptidase 4	IC 50 (nM)	8	N/A	N/A	Details