Abstract
Mebendazole is a well known anti-helimintic and belongs to the benzimidazole group of medicines. In order to achieve better medicinal results, i.e. enhanced activity and low toxicity, structural modifications are made in the existing drugs. Some 5-benzoyl-N-[1-(alkoxyphthalimido) benzimidazol-2-yl] carbamic acid methyl ester(3a-c)and 5-benzoyl-N-[1-(2,3-bis oxyphthalimido∕oxysuccinimido propyl benzimidazol-2-yl) carbamic acid methyl ester(7a-b)have been synthesized from two different routes. Structures of the compounds have been established on the basis of elemental analysis and spectral studies. All the synthesized compounds(3a-c)and(7a-b)were assayedin vitrofor antimicrobial activity against mebendazole (itself) and standard [ciprofloxacin (antibacterial) and fluconazole (antifungal)].
Highlights
Mebendazole belongs to the family of medicines called anthelmintics, is especially useful against whipworm infection
Mebendazole was found effective in decreasing the concentration of a strain of cytochromes P450 (CYP) in primary culture of swine (Sus scrofa f. domestica) hepatocytes[3]
Mebendazole has been tested as antigiradial agents, which acts by especially inhibiting tubulin polymerisation caused by Giardia lambia, a parasite survives in the intestinal tracts of human and other mammals as microtubule assembly[5]
Summary
Mebendazole (me-BEN-da-zole) belongs to the family of medicines called anthelmintics, is especially useful against whipworm infection. Sodium salt of 5-Benzoyl(1H)benzimidazol-2-yl-carbamic acid methyl ester (1) Sodium salt of mebendazole (1) (3.17 gm, 0.01 mole) was suspended in DMF, phthalimidoxyethylbromide (2.69gm, 0.01 mole) in DMF was added with constant stirring on a powerful magnetic stirrer.
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