الفهرس | Only 14 pages are availabe for public view |
Abstract The thesis involves the design and synthesis of some new coumarin derivatives with biological investigation for their anti-inflammatory. analgesic and antimicrobial activities. Thus, it prefaced by a brief account about the biological activities and chemical synthetic methods for different reported coumarin derivatives. Furthermore, the thesis declare the design and synthesis of a new series of 4-methyl-7-methoxycomarin derivatives; 36 new compounds (4 intermediate and 32 new targeted compounds), were prepared starting from 2-((4-methyl-2-oxo-2h-chromen-7-yl)oxy) acetohydrazide. compound 4. The purity of all new compounds was checked by TLC and eluidation of their structures was comfirmed by IR. 1H. 13C NMR, HRMS and some representatives by El-MS along with elemental microanalyses. Anti-inflammatory activity of all newly synthesized compounds was evaluated in vivo; the results showed that most of the tested compounds exhibited significant anti-inflammatory activity in comparison to indomethacin as a reference drug. Moreover, copounds 81, 12g were more active than indomethacin giving 117% and 113% anti-infakkatory activity of indomethacin after 5 h respectively. Compounds 6a, 8g, 8i, 8k and 81 were tested for their analgesic effects in comparison to indomethacin as a reference drug. Compounds 6a and 8i showed activity comparable to the reference drug. Compounds 6a, 8d and 8I were examined for their effect on gastric mucosa and showed no gastric ulcerrogenic effect up to oral dose 60 mg/Kg. Moreover, LD50 of compounds 6a and 8I were determined; they exhibited no-toxic effect up to 240 and 300 mg/kg (i.p.) respectively. |