In vitro PAI-1 inhibitory activity of oxalamide derivatives

Mukul R Jain; Shankar Shetty; Ganes Chakrabarti; Vrajesh Pandya; Ajay Sharma; Bhavesh Parmar; Soma Srivastava; Mehul Raviya; Hitesh Soni; Pankaj R Patel

doi:10.1016/j.ejmech.2007.05.011

In vitro PAI-1 inhibitory activity of oxalamide derivatives

Eur J Med Chem. 2008 Apr;43(4):880-4. doi: 10.1016/j.ejmech.2007.05.011. Epub 2007 Jun 3.

Authors

Mukul R Jain¹, Shankar Shetty, Ganes Chakrabarti, Vrajesh Pandya, Ajay Sharma, Bhavesh Parmar, Soma Srivastava, Mehul Raviya, Hitesh Soni, Pankaj R Patel

Affiliation

¹ Zydus Research Centre, Sarkhej-Bavla NH No. 8A, Moraiya, Ahmedabad-382210, Gujarat, India. mukul.jain@zyduscadila.com

PMID: 17664030
DOI: 10.1016/j.ejmech.2007.05.011

Abstract

A number of oxalamide derivatives have been synthesized and evaluated for PAI-1 inhibitory activity. In vitro PAI-1 inhibitory activities of oxalamide derivatives are evaluated by chromogenic assay. Few compounds have shown significant PAI-1 inhibitory activity.

MeSH terms

Amides / chemistry*
Humans
Inhibitory Concentration 50
Oxamic Acid / chemistry
Oxamic Acid / pharmacology*
Plasminogen Activator Inhibitor 1 / chemistry*
Plasminogen Activator Inhibitor 1 / metabolism*
Serine Proteinase Inhibitors / chemistry*
Serine Proteinase Inhibitors / metabolism*
Tissue Plasminogen Activator / metabolism

Substances

Amides
Plasminogen Activator Inhibitor 1
Serine Proteinase Inhibitors
Tissue Plasminogen Activator
Oxamic Acid