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