Abstract

Synthesis and biological evaluation of some new coumarin derivatives as potential antimicrobial, analgesic and anti-inflammatory agents

Author(s): Mohammed A. I. Elbastawesy a , Bahaa G. M. Youssif b,c , Mostafa H. Abdelrahman a and Alaa M. Hayallah * b,d

A new series of 4-methyl-7-methoxycoumarin derivati ves linked triazoles and oxadiazole were prepared s tarting from 2-((4-methyl-2-oxo-2H-chromen-7-yl)oxy) acetoh ydrazide, compound 4 . The purity of all new compounds was checked by TLC and elucidation of their structures was confirmed by IR , 1 H and 13 C NMR along with High Resolution Mass Spectrometry ( HRMS ). All the target compounds were evaluated for their possible anti- inflammatory activities. The result showed that mos t of the tested compounds exhibited significant ant i-inflammatory activity in comparison to indomethacin as a referen ce drug. The compound 8l was the most active one. Compounds 6a , 8g , 8i , 8k and 8l were tested for their analgesic effects in compari son to indomethacin as a reference drug. Compounds 6a and 8i showed activity comparable to the reference drug. Compounds 6a , 8d and 8l were examined for their effect on gastric mucosa and showed no ga stric ulcerogenic effect at dose 60 mg/Kg. Moreover , LD 50 of compounds 6a and 8l were determined; they exhibited no-toxic effect up to 240 and 300 mg/kg (i.p.) respectively. Finally, compounds 7 and 8a-8j were evaluated for their possible antimicrobial ac tivity. Most of the tested compounds showed moderate to good antimicrobial act ivity against most of the strains used in compariso n with ciprofloxacin and fluconazole as reference drugs.

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