The design of potent and selective inhibitors of thrombin utilizing a piperazinedione template: part 2

W L Cody; C E Augelli-Szafran; K A Berryman; C Cai; A M Doherty; J J Edmunds; J X He; L S Narasimhan; J Penvose-Yi; J S Plummer; S T Rapundalo; J R Rubin; C A Van Huis; L Leblond; P D Winocour; M A Siddiqui

doi:10.1016/s0960-894x(99)00419-9

The design of potent and selective inhibitors of thrombin utilizing a piperazinedione template: part 2

Bioorg Med Chem Lett. 1999 Sep 6;9(17):2503-8. doi: 10.1016/s0960-894x(99)00419-9.

Authors

W L Cody¹, C E Augelli-Szafran, K A Berryman, C Cai, A M Doherty, J J Edmunds, J X He, L S Narasimhan, J Penvose-Yi, J S Plummer, S T Rapundalo, J R Rubin, C A Van Huis, L Leblond, P D Winocour, M A Siddiqui

Affiliation

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

PMID: 10498197
DOI: 10.1016/s0960-894x(99)00419-9

Abstract

Potent and selective thrombin inhibitors have been prepared with a piperazinedione template and L-amino acids. Likewise, incorporation of D-amino acids led to potent inhibitors with a novel mode of binding. Herein, the structure activity relationships and structural aspects of these compounds will be described.

MeSH terms

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

Substances

Antithrombins
Piperazines