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study the toxicity and anticancer activity of some new derivatives of mefenamic acid
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نویسنده
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sabah ali amad ,mhaibes raed muslim ,jarallah aziz latif ,salman salim dawood ,al-rawi muna sameer
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منبع
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journal of medicinal and chemical sciences - 2023 - دوره : 6 - شماره : 5 - صفحه:1000 -1009
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چکیده
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The new 1,3-oxazepine derivatives (iva-d) were manufactured from the response of n-arylhydrazone (iii) based on mefenamic acid with various cyclic carboxylic acid anhydrides such as (succinic, maleic, phthalic, and 3- nitrophthalic) anhydride by using dry benzene under reflex via (2+5) cycloaddition reaction. these compounds 1,3-oxazepine (iv) were obtained via a four-steps- sequence reactions in good yields. condensation reaction of mefenamic acid with chloroacetyl chloride to give 2 -[2-chloro-n-(2,3- dimethylphenyl) acetamido] benzoic acid (i), which on amination with hydrazine hydrate in ethanol to give a corresponding acid hydrazid (ii). the acid hydrazide was used as the starting materials on condensation with syringe aldehyde afforded newly n-arylhydrazone (iii) in a good yield. finally, the later compound reacted with different type of acid anhydrides to get new derivatives of 1,3-oxazepine. the new compounds were characterized by using ft-ir, 1h-nmr, and mass spectroscopy. in addition, the potential antibacterial activities for the certain compounds were investigated by using three species of bacteria: staphylococcus aureus, klebsiella pneumoniae, and escherichia coli which most of the target derivatives have exhibited a good efficacy compared with ampicillin (as antibacterial). besides the cytotoxic effect by using various concentrations of the derivatives (ivc) and (ivd) were assessed by human breast carcinoma cells (mcf-7), which have been exhibited a high effect on the concentration of 400 μl/ml with ic50 =80.20 and ic50=82.80. a tiered approach to investigate the toxicity utilized mice to estimate its acute toxicity and the result confirmed the non-toxicity of these compounds
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کلیدواژه
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mefenamic acid ,cycloaddition reaction ,pro-drug moieties ,toxicity activity ,anticancer activity
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آدرس
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directorate of education qalaat sukkar, al-fajr preparatory school for boys, iraq, misan university, college for medicine, department of biochemistry, iraq, al-esraa university college, department of medical labs, iraq, ashur university college, department of pharmacy, iraq, university of baghdad, college of education for pure science ibn al- haitham, department of chemistry, iraq
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پست الکترونیکی
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mona.s.s@ihcoedu.uobaghdad.edu.iq
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Authors
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