| Literature DB >> 10340621 |
J Ambler1, L Brown, X L Cockcroft, M Grütter, J Hayler, D Janus, D Jones, P Kane, K Menear, J Priestle, G Smith, M Talbot, C V Walker, B Wathey.
Abstract
The optimisation of the P2 pharmacophore in a series of thrombin inhibitors is described. The interaction of a number of piperidine P2 functionalities with lysine 60G of thrombin is explored with reference to the crystal structure of inhibitor enzyme complexes. A primary ion-dipole interaction between the terminal P2 side chain group and lysine 60G is evoked to explain the SAR in this series.Entities:
Mesh：
Substances：
Year: 1999 PMID： 10340621 DOI： 10.1016/s0960-894x(99)00172-9
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823