The design of potent and selective inhibitors of thrombin utilizing a piperazinedione template: part 1

W L Cody; C Cai; A M Doherty; J J Edmunds; J X He; L S Narasimhan; J S Plummer; S T Rapundalo; J R Rubin; C A Van Huis; Y St-Denis; P D Winocour; M A Siddiqui

doi:10.1016/s0960-894x(99)00418-7

The design of potent and selective inhibitors of thrombin utilizing a piperazinedione template: part 1

Bioorg Med Chem Lett. 1999 Sep 6;9(17):2497-502. doi: 10.1016/s0960-894x(99)00418-7.

Authors

W L Cody¹, C Cai, A M Doherty, J J Edmunds, J X He, L S Narasimhan, J S Plummer, S T Rapundalo, J R Rubin, C A Van Huis, Y St-Denis, P D Winocour, M A Siddiqui

Affiliation

¹ Parke-Davis Pharmaceutical Research, Division of Warner-Lambert Company, Ann Arbor, MI 48105, USA.

PMID: 10498196
DOI: 10.1016/s0960-894x(99)00418-7

Abstract

Utilizing X-ray crystallography and molecular modeling, highly potent and selective peptidomimetic thrombin inhibitors have been designed containing a rigid piperazinedione template. The synthesis and biological activity of these compounds will be described.

MeSH terms

Antithrombins / chemical synthesis*
Antithrombins / chemistry
Antithrombins / pharmacology
Crystallography, X-Ray
Drug Design*
Models, Molecular
Piperazines / chemistry*

Substances

Antithrombins
Piperazines