Evaluation of genetic damage induced by a nitroimidazole derivative in human lymphocytes: Tinidazole (TNZ)

Nigro, Marcela M. López; Gadano, Andrea; Carballo, Marta A.

doi:10.1016/s0887-2333(01)00010-8

Cited by 17 publications

(6 citation statements)

References 17 publications

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“…Ornidazole [1‐(2‐hydroxy‐3‐chloro)‐propyl‐2‐methyl‐5‐nitroimidazole] is used for the treatment and prophylaxis of infections by anaerobic and microaerophilic bacteria and protozoa 1 . It is more effective than metronidazole and tinidazole against amoebiasis or dientamoebiasis, and as effective as metronidazole in trichomoniasis 2–4 . The main side‐effects of ornidazole are nausea, vomiting, spermatotoxicity and central nerve toxicity 5–7 .…”

Section: What Is Known and Objectivementioning

confidence: 99%

Investigation of chiral inversion and pharmacokinetics of laevo-ornidazole by high-performance liquid chromatography

Zhang

Guo

et al. 2012

Journal of Clinical Pharmacy and Therapeutics

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We present the first reported method for the chiral separation of ornidazole in human plasma. We demonstrate the absence of chiral inversion of laevo-ornidazole in vivo. Given the absence on in vivo chiral inversion, we also report and validate a simplified non-chiral method for the determination of laevo-ornidazole. We show that although food can affect the absorption rate of laevo-ornidazole, the extent was unaffected.

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Section: What Is Known and Objectivementioning

confidence: 99%

Investigation of chiral inversion and pharmacokinetics of laevo-ornidazole by high-performance liquid chromatography

Zhang

Guo

et al. 2012

Journal of Clinical Pharmacy and Therapeutics

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“…Among these, metronidazole and tinidazole are well-known antimicrobial drugs as well as sensitizers of hypoxic tumors in conjunction with radiotherapy. The biological activity of nitroimidazole derivatives is dependent upon the nitro group reduction process due to the formation of active intermediate species that interact with DNA causing biochemical damage [3][4][5]. The small molecular size and low extent of protein binding of nitroimidazoles favor their distribution throughout the body.…”

Section: Introductionmentioning

confidence: 99%

Voltammetric determination of tinidazole in pharmaceutical tablets using carbon paste electrode

Taye¹,

Amare²

2016

Bull. Chem. Soc. Eth.

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ABSTRACT. Cyclic voltammetry was used to study the electrochemical behavior of tinidazole at carbon paste electrode. Tinidazole showed an irreversible reduction peak at about -440 mV. The differential pulse voltammetric peak current of tinidazole showed linear dependence on concentration in the range 5.0-200 μM with LOD and LOQ of 5.1  10 -7 and 1.7  10 -6 μM, respectively. Relative to most of the reported works on the determination of tinidazole, the developed method using carbon paste electrode which is an environmentally friendly, cheap, and simple working electrode exhibited linear dependence of peak current on concentration in the lower concentration region with relatively low LOD. Excellent recovery results with low % RSD for spiked standard tinidazole in tablet samples showed the potential applicability of the developed method for the determination of tinidazole in real samples.

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“…Although a number of different protozoa may cause these symptoms, E. histolytica is the most commonly reported one. Metronidazole (MNZ) is an important drug in the treatment of several types of illnesses caused by protozoa, as well as anaerobic bacteria. − However, critical lateral effects have been described, i.e., neurological alterations produced by interaction of the drug with the central nervous system and impairment of the cardiac rhythm due to chelation of MNZ with calcium ions. MNZ also induces certain tumors in rodents and is mutagenic toward bacteria. − According to the International Agency for Research on Cancer (IARC), MNZ is classified in the 2B group, i.e., potentially carcinogenic to humans, and proved to be carcinogenic to animals…”

Section: Introductionmentioning

confidence: 99%

Dioxo- and Oxovanadium(V) Complexes of Thiohydrazone ONS Donor Ligands: Synthesis, Characterization, Reactivity, and Antiamoebic Activity

et al. 2006

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As a contribution to the development of novel vanadium complexes with pharmacologically interesting properties, two neutral dioxovanadium(V) complexes [VO2(Hpydx-sbdt)] (1) and [VO2(Hpydx-smdt)] (3) [H2pydx-sbdt (I) and H2pydx-smdt (II) are the Schiff bases derived from pyridoxal and S-benzyl- or S-methyldithiocarbazate] have been synthesized by the reaction of [VO(acac)2] and the potassium salts of the ligands in methanol followed by aerial oxidation. Heating of the methanolic solutions of these complexes yields the oxo-bridged binuclear complexes [{VO(pydx-sbdt)}2mu-O] (2) and [{VO(pydx-smdt)}2mu-O] (4). The crystals and molecular structures of 1, 3 x 1.5H2O, and 4 x 2CH3OH have been determined, confirming the ONS binding mode of the dianionic ligands in their thioenolate form. The ring nitrogen of the pyridoxal moiety is protonated in complexes 1 and 3. Acidification of 1 and 3 with HCl dissolved in methanol afforded oxohydroxo complexes, while in a methanolic KOH solution, the corresponding dioxo species K[VO2(pydx-sbdt/smdt)] are formed. Treatment of 1 and 3 with H2O2 yields (unstable) oxoperoxovanadium(V) complexes, the formation of which has been established spectrophotometrically. In vitro antiamoebic activities (against HM1:1MSS strain of Entamoeba histolytica) were established for all of the dioxo- and oxovanadium(V) complexes. The complexes 1, 2, and 4 were more effective than metronidazole, a commonly used drug against amoebiasis, suggesting that oxovanadium(V) complexes derived from thiohydrazones may open a new dimension in the therapy of amoebiasis.

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Evaluation of genetic damage induced by a nitroimidazole derivative in human lymphocytes: Tinidazole (TNZ)

Cited by 17 publications

References 17 publications

Investigation of chiral inversion and pharmacokinetics of laevo-ornidazole by high-performance liquid chromatography

Investigation of chiral inversion and pharmacokinetics of laevo-ornidazole by high-performance liquid chromatography

Voltammetric determination of tinidazole in pharmaceutical tablets using carbon paste electrode

Dioxo- and Oxovanadium(V) Complexes of Thiohydrazone ONS Donor Ligands: Synthesis, Characterization, Reactivity, and Antiamoebic Activity

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