Letters in Drug Design & Discovery

G. Perry
University of Texas
San Antonio, TX
USA
Email: lddd@benthamscience.org

Back

Synthesis and Chymotrypsin Inhibitory Activity of Substituted Oxazolones

Author(s): Khalid Mohammed Khan, Uzma Rasool Mughal, Muhammad Arif Lodhi, Muhammad Iqbal Choudhary.

Abstract:

A variety of oxazolones (3-18) with structural variation at C-2 and C-4 were synthesized and evaluated as chymotrypsin inhibitors. The synthesized compounds showed varying degree of chymotrypsin inhibitory activity ranging IC50 values from 12.62 ± 1.32 - 126.57 ± 1.06 μM, if compared to standard chymostatin (IC50 = 7.01 ± 0.1 μM). Compounds 3,9,10,13,14, and 15 have IC50 values 17.03 ± 0.78, 69.05 ± 1.48, 12.62 ± 1.32, 17.29 ± 0.93, 126.57 ± 1.06, and 31.55 ± 1.31 μM, respectively. This study reveals that the substitution of functional group (s) at C-2 and C-4 positions plays a vital role in the activity of this series of compounds. The size and electron donating or withdrawing effects of substituents influenced the activity.

Keywords: Synthesis, Oxazolone Derivatives, Chymotrysin inhibition

Order Reprints Order Eprints Rights & PermissionsPrintExport

Article Details

VOLUME: 5
ISSUE: 1
Year: 2008
Page: [52 - 56]
Pages: 5
DOI: 10.2174/157018008783406624