Glucuronidation of 3'-azido-3'-deoxythymidine: Human and rat enzyme specificity
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Stability-indicating micellar liquid chromatography method for three novel derivatives of zidovudine in aqueous and simulated gastric and intestinal fluids matrices
2011, Journal of Chromatography ACitation Excerpt :Despite worldwide attempts underway to develop chemotherapeutic agents that are effective against HIV, 3′-azido-2′,3′-dideoxythymidine, or zidovudine (AZT) (Fig. 1), the first drug approved for the treatment of AIDS patients [12], is still one of the most potent active agents against HIV, and is used as a primary option in AIDS treatment in combination with other HIV inhibitors. Nevertheless, utility of AZT is limited by its toxic effect on bone marrow [13], hepatic abnormalities [14], limited brain uptake [15], short half-life time in plasma [16], high susceptibility to catabolism [17], general myopathy [18], lipoatrophy [19] and the rapid progress of resistance by HIV-1 [20]. For these reasons, numerous chemical strategies have been developed by medicinal scientists to design analogues or prodrugs of AZT to increase its therapeutic efficacy [21].
Nucleoside and nucleotide HIV reverse transcriptase inhibitors: 25 years after zidovudine
2010, Antiviral ResearchNatural and synthetic inhibitors of UDP-glucuronosyltransferase
2001, Pharmacology and TherapeuticsLiver Slices as a Model in Drug Metabolism
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