Synthesis and Chymotrypsin Inhibitory Activity of Substituted Oxazolones

Title: Synthesis and Chymotrypsin Inhibitory Activity of Substituted Oxazolones

Volume: 5 Issue: 1

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

Affiliation:

Keywords: Synthesis, Oxazolone Derivatives, Chymotrysin inhibition

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.

Cite this article as:

Khan Mohammed Khalid, Mughal Rasool Uzma, Lodhi Arif Muhammad and Choudhary Iqbal Muhammad, Synthesis and Chymotrypsin Inhibitory Activity of Substituted Oxazolones, Letters in Drug Design & Discovery 2008; 5 (1) . https://dx.doi.org/10.2174/157018008783406624