Potent and selective bicyclic lactam inhibitors of thrombin: Part 3: P1' modifications.

Janet S. Plummer,Kent Alan Berryman,Cuiman Cai,Wayne L. Cody,John T. M. DiMaio,Annette Marian Doherty,Scott R. Eaton,Jeremy J. Edmunds,Debra R. Holland,D Lafleur,Sophie Levesque,Lakshmi S. Narasimhan,J. Ronald Rubin,Stephen T. Rapundalo,M. Arshad Siddiqui,A. Susser,Yves St-Denis,Peter D. Winocour

Potent and selective bicyclic lactam inhibitors of thrombin: Part 3: P1' modifications.

1999

Janet S. Plummer
Kent Alan Berryman
Cuiman Cai
Wayne L. Cody
John T. M. DiMaio
Annette Marian Doherty
Scott R. Eaton
Jeremy J. Edmunds
Debra R. Holland
D Lafleur
Sophie Levesque
Lakshmi S. Narasimhan
J. Ronald Rubin
Stephen T. Rapundalo
M. Arshad Siddiqui
A. Susser
Yves St-Denis
Peter D. Winocour

Abstract The synthesis and antithrombotic activity of a series of nonpeptide bicyclic thrombin inhibitors are described. We have explored the SAR around the P1′ site. Modification of the P1′ site has been found to affect potency and selectivity.

Keywords:

Stereochemistry
Organic chemistry
Thrombin
Chemical synthesis
Discovery and development of direct thrombin inhibitors
Bicyclic molecule
Antithrombotic
Enzyme inhibitor
Chemistry
Lactam
Active site

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