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Authors: Abbas, Waseem
Keywords: Pharmaceutical Chemistry
Issue Date: 2021
Series/Report no.: ;6255
Abstract: Metronidazole is a 5- nitro imidazole that has become the cornerstone in the treatment of worldwide anaerobic infections and ranks amongst the essential medicines as elucidate by WHO. In 1959, it was developed primarily for the treatment of Trichomoniasis, a genital tract infection caused by a microaerophilic parasite, Trichomonas vaginalis, which at that time was notoriously hard to handle. Without any unique pathways, such as transporters, metronidazole absorption occurs, but it relies on metabolic activity to maintain an energetic membrane as such, it is a pro drug that is poorly reactive, but if the nitro group is reduced, metronidazole is converted into a reactive group. Enteric protozoan infection is the most common type of infection throughout the worldwide and is consequential cause of morbidity and mortality. Ester is a major class of organic compounds that contain alcohols and organic and inorganic acids when it reacts with water. Metronidazole esterification was performed with the acid containing (COOH) group, ethanol used as a solvent and mineral acid as a catalyst. 12 ester derivatives of metronidazole formed through fisher esterification. The physical characterization was carried out by testing the solubility, melting point, color and physical state of the derivatives. The chemical characterization was carried out by studying the FTIR and NMR spectra. Antioxidant and anti-microbial activity have been found in these derivatives. Among all derivatives MT-14 and MT-08 manifested excessive antioxidant activity 97%, 88% sequentially in correlation of standard ascorbic acid (97%). Metronidazole was used as standard for antimicrobial activity. Among all derivatives MT-1, MT-3, MT-4 and MT-6 had showed comparable activity as compared to standard metronidazole. But derivative MT-13 showed slightly higher microbial activity as compared to standard metronidazole.
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