SYNTHESIS, BIOLOGICAL EVALUATION AND IN SILICO ADME PREDICTIONS OF SOME NEW COUMARIN-ACETAMIDE DERIVATIVES AS POTENT ANTI-INFLAMMATORY AGENTS

Elbastawesy, Mohammed A. I.; Morcoss, Martha M.; Abdelrahman, Mostafa H.; Youssif, Bahaa G.M.; Hayallah, Alaa M.

doi:10.21608/bfsa.2021.207161

SYNTHESIS, BIOLOGICAL EVALUATION AND IN SILICO ADME PREDICTIONS OF SOME NEW COUMARIN-ACETAMIDE DERIVATIVES AS POTENT ANTI-INFLAMMATORY AGENTS

Document Type : Original Article

Authors

¹ Pharmaceutical Organic Chemistry Department, Faculty of Pharmacy, Al-azhar University, Assiut Branch 71524, Assiut, Egypt.

² Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Nahda University, 62513 Beni-Suef, Egypt

³ Pharmaceutical Organic Chemistry Department, Faculty of Pharmacy, Assiut University, Assiut 71526, Assiut, Egypt

⁴ Pharmaceutical Chemistry Department, Faculty of Pharmacy, Sphinx University, New Assiut, Egypt

10.21608/bfsa.2021.207161

Abstract

A new series of 4-methyl-7-methoxycoumarin derivatives linked with three amide groups
were prepared starting from 2-((4-methyl-2-oxo-2H-chromen-7-yl)oxy) acetohydrazide,
compound 4. TLC was used to ensure the purity of all new compounds, and IR, 1H NMR, and
mass spectrometry, as well as elemental microanalyses, were used to confirm their structures.
All of the target compounds were tested for anti-inflammatory activity. The results showed that
most of the tested compounds exhibited significant anti-inflammatory activity in comparison to
indomethacin (INM) as a reference drug. The results revealed that compound 8g was the most
active one exceeding the activity of the reference INM. Moreover, compounds 8f and 8k showed
approximately the same results as INM after 5 hr. In silico ADME prediction investigations also
forecasting the drug-like characters of these compounds .