SYNTHESIS, BIOLOGICAL EVALUATION AND IN SILICO ADME PREDICTIONS OF SOME NEW COUMARIN-ACETAMIDE DERIVATIVES AS POTENT ANTI-INFLAMMATORY AGENTS | ||||
| Bulletin of Pharmaceutical Sciences Assiut University | ||||
| Article 14, Volume 44, Issue 2, December 2021, Page 427-441 PDF (894.64 K) | ||||
| Document Type: Original Article | ||||
| DOI: 10.21608/bfsa.2021.207161 | ||||
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| Authors | ||||
Mohammed A. I. Elbastawesy   1; Martha M. Morcoss2; Mostafa H. Abdelrahman1; Bahaa G.M. Youssif3; Alaa M. Hayallah3, 4
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| 1Pharmaceutical Organic Chemistry Department, Faculty of Pharmacy, Al-azhar University, Assiut Branch 71524, Assiut, Egypt. | ||||
| 2Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Nahda University, 62513 Beni-Suef, Egypt | ||||
| 3Pharmaceutical Organic Chemistry Department, Faculty of Pharmacy, Assiut University, Assiut 71526, Assiut, Egypt | ||||
| 4Pharmaceutical Chemistry Department, Faculty of Pharmacy, Sphinx University, New Assiut, Egypt | ||||
| 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 . | ||||
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