1,4-Diazepane-2,5-diones as novel inhibitors of LFA-1

Sompong Wattanasin; Joerg Kallen; Stewart Myers; Qin Guo; Michael Sabio; Claus Ehrhardt; Rainer Albert; Ulrich Hommel; Gisbert Weckbecker; Karl Welzenbach; Gabriele Weitz-Schmidt

doi:10.1016/j.bmcl.2004.11.072

1,4-Diazepane-2,5-diones as novel inhibitors of LFA-1

Bioorg Med Chem Lett. 2005 Feb 15;15(4):1217-20. doi: 10.1016/j.bmcl.2004.11.072.

Authors

Sompong Wattanasin¹, Joerg Kallen, Stewart Myers, Qin Guo, Michael Sabio, Claus Ehrhardt, Rainer Albert, Ulrich Hommel, Gisbert Weckbecker, Karl Welzenbach, Gabriele Weitz-Schmidt

Affiliation

¹ Novartis Institutes for BioMedical Research, Cambridge, MA 02139, USA. sompong.wattanasin@pharma.novartis.com

PMID: 15686945
DOI: 10.1016/j.bmcl.2004.11.072

Abstract

1,4-Diazepane-2,5-diones (2) are found to be a new class of potent LFA-1 inhibitors. The synthesis, structure, and biological evaluation of these 1,4-diazepine-2,5-diones and related derivatives are described.

MeSH terms

Heterocyclic Compounds, 4 or More Rings / chemical synthesis*
Heterocyclic Compounds, 4 or More Rings / pharmacology
Humans
Intercellular Adhesion Molecule-1 / metabolism
Ketones / chemical synthesis*
Ketones / pharmacology
Lymphocyte Function-Associated Antigen-1 / drug effects*
Lymphocyte Function-Associated Antigen-1 / metabolism
Protein Binding / drug effects
Stereoisomerism
Structure-Activity Relationship

Substances

Heterocyclic Compounds, 4 or More Rings
Ketones
Lymphocyte Function-Associated Antigen-1
Intercellular Adhesion Molecule-1