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Saturday, July 25, 2020 | History

2 edition of Genotoxicity of nitroheterocyclic drugs. found in the catalog.

Genotoxicity of nitroheterocyclic drugs.

Michael Cheshire

Genotoxicity of nitroheterocyclic drugs.

by Michael Cheshire

  • 238 Want to read
  • 36 Currently reading

Published by PEL in London .
Written in English


Edition Notes

Thesis (M.Phil.) - Polytechnic of East London, Chemotherapy Research Unit and Department of Molecular Radiology, Cancer Research Campaign, 1987.

ID Numbers
Open LibraryOL13792847M

method in drug formulation processes, alkyl halides exist as impurities in several drugs (Sobol et al., ; Elder et al., a). Genotoxicity profile. Background: Nitro-derivatives of heterocyclic compounds were used as active agents against pathogenic microorganisms. A set of 4- and 5-nitroimida.

  Nitroheterocyclic compounds are more efficacious than CYP51 inhibitors against Trypanosoma cruzi: implications for Chagas disease drug discovery and development Carolina B. Moraes, a, 1, 2 Miriam A. Giardini, 1 Hwayoung Kim, 1 Caio H. Franco, 2 Adalberto M. Araujo-Junior, 2 Sergio Schenkman, 3 Eric Chatelain, 4 and Lucio H. Freitas. What is genotoxicity, and why should we worry about it? A genotoxin is a substance that either permanently alters DNA (mutagenicity) or alters a cell’s ability to regulate DNA structure and content. Mutation or damage to DNA may or not result in a permanent change its content or structure, depending on several factors including DNA repair, metabolism, apoptosis, and oxidative stress defence.

Abstract. Genotoxicity tests are designed to detect the genetic damage by various mechanisms. Several guidelines have provided various tests to be conducted for testing the genotoxicity and each of the regulatory agencies around the world have developed their own requirements for mutagenicity, without realizing that the products developed or registered in one country are also going to be. While there are dedicated guidelines for industry regarding the assessment of the genotoxic potential of new pharmaceuticals and impurities, and the general safety assessment of major drug metabolites, only limited guidance exists on the assessment of potential genotoxic minor drug metabolites. In this Perspective, we discuss challenges associated with assessing the genotoxic potential of.


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Genotoxicity of nitroheterocyclic drugs by Michael Cheshire Download PDF EPUB FB2

1. Introduction. The introduction of nitro-substituted heterocyclic drugs, such as nitroimidazoles and nitrofurans, heralded a new era. 5-Nitrofurans and 2- and 5-nitroimidazoles are the classes of nitroheterocyclic drugs most used in the treatment of infections caused by anaerobic bacteria and a range of pathogenic protozoan parasites [1–4].

Cited by: Nitroheterocyclic compounds are widely used as therapeutic agents against a variety of protozoan and bacterial infections. However, the literature on these compounds, suspected of being carcinogens, is widely controversial. In this study, cytotoxic and genotoxic potential of three drugs, Nifurtimox (NFX), Benznidazole (BNZ), and Metronidazole (MTZ) was Genotoxicity of nitroheterocyclic drugs.

book by different by: Genotoxicity Revaluation of Three Commercial Nitroheterocyclic Drugs: Nifurtimox, Benznidazole, and Metronidazole Article (PDF Available) in Journal of Parasitology Research (1)   This paper describes a genotoxicity evaluation of fexinidazole (1H-imidazole,1-methyl[[4-methylthio) phenoxy] methyl] 5-nitroimidazole), a 2-substituted 5-nitroimidazole, rediscovered by the Drugs for Neglected Diseases initiative (DNDi) after extensive compound mining of drug companies and published by:   Genotoxicity Revaluation of Three Commercial Nitroheterocyclic Drugs: Nifurtimox, Benznidazole, and Metronidazole Annamaria Buschini, 1 Lisa Ferrarini, 1 Susanna Franzoni, 1 Serena Galati, 1 Mirca Lazzaretti, 1 Francesca Mussi, 1 Cristina Northfleet de Albuquerque, 2 Tânia Maria Araújo Domingues Zucchi, 3 and Paola Poli 1, *.

W.J. Rogers, in Sterilisation of Biomaterials and Medical Devices, Genotoxicity – ISO –3. Genotoxicity testing evaluates gene mutations, changes in chromosomes or DNA and gene toxicities caused by by-products or compounds over an extended period of time. The International Organization for Standardization (ISO) standard –3 outlines tests for genotoxicity.

Genotoxicity Revaluation of Three Commercial Nitroheterocyclic Drugs: Nifurtimox, Benznidazole, and Metronidazole By Annamaria Buschini, Lisa Ferrarini, Susanna Franzoni, Serena Galati, Mirca Lazzaretti, Francesca Mussi, Cristina Northfleet de Albuquerque, Tânia.

Dockets Management Food and Drug Administration Fishers Lane, Rm Rockville, MD All written comments should be identified with this document's docket number: FDAD Keywords:Prodrugs, nitro-compounds, metronidazol, nitrofurazone, genotoxicity, physico-chemical properties, nitroheterocyclic compounds, half-life, nitroimidazoles, Chagas disease.

Abstract: In therapeutics research, the nitro compounds are part of an important group of drugs with multiple pharmacological activities. However, in drug design. in drugs followed by monitoring and control at very low levels to ensure safety to the public [2,3].

Sources of Genotoxic Impurities Genotoxic impurities can get incorporated into drug substances through the various sources, the major source is the starting material used in the synthesis of drug. The relatively high prescription rates for this drug clearly demonstrate the need for an objective assessment of the potential biohazards posed by MZ in man.

The major findings relating to the biotransformation, genotoxicity and carcinogenicity of MZ are reviewed in this paper. Pharmacokinetics Similarly, ROS have been implicated in genotoxicity caused by particles and fibers.

Genotoxicity of nonfibrous and fibrous particles is characterized by high production of ROS from inflammatory cells. Genotoxic chemotherapy. Genotoxic chemotherapy is the treatment of cancer with the use of one or more genotoxic drugs.

measuring the extend of genotoxicity have also been discussed such as chromosomal aberration test and micronucleus assay. Finally a brief account on the drugs being used in present days, and also some plant products which show anti mutagenic effects have been emphasized.

Keywords: Genotoxicity, Mutagen, Mutations, Aberrations. INTRODUCTION. Genotoxicity Revaluation of Three Commercial Nitroheterocyclic Drugs: Nifurtimox, Benznidazole, and Metronidazole By T&, Cristina Northfleet de Albuquerque, Francesca Mussi, Mirca Lazzaretti, Susanna Franzoni, Serena Galati, Lisa Ferrarini, Annamaria Buschini and Paola Poli.

Figure 4: Flow chart on Genotoxicity Testing [26]. Purpose of genotoxicity assays Assays even though inexpensive, have high statistical power and can be reproduced and have the ability to detect a wide variety of genotoxic end-points.

It also allows the detection of a drug’s potential to cause genotoxicity even in the early stage of drug. Office of Communications Division of Drug Information, WO51, Room Center for Drug Evaluation and Research Food and Drug Administration New Hampshire Ave., Silver Spring, MD genotoxicity as “a broad term that refers to any deleterious change in the genetic material regardless of the mechanism by which the change is induced.” Genotoxic impurities have also been defined as an “impurity that has been demonstrated to be genotoxic in an appropriate genotoxicity test model, e.g., bacterial gene mutation (Ames).

Nitroheterocyclic compounds are more efficacious than CYP51 inhibitors against Trypanosoma cruzi: implications for Chagas disease drug discovery and development Carolina B.

Moraes 1, 2 Miriam A. Genotoxicity tests are designed to detect compounds that directly or indirectly cause these types of genetic damage by different mechanisms. Regulatory agencies require a standard battery of genotoxicity studies prior to authorization to conduct Phase I clinical trials with a new drug.

Federal Institute for Drugs and Medical Devices (BfArM), Bonn, Germany. Search for more papers by this author Book Editor(s): Nicolay Ferrari. Search for more papers by this author the Subcommittee believes that genotoxicity testing of new ONs is warranted because modified monomers could be liberated from a metabolized ON and.

Hematopoietic stem/progenitor cells (HSPCs) are susceptible to benzene-induced genotoxicity. However, little is known about the mechanism of DNA damage response affecting lineage-committed progenitors for myeloid, erythroid, and lymphoid.

Here, we investigated the genotoxicity of a benzene metabolite, 1,4-benzoquinone (1,4-BQ), in HSPCs using oxidative stress and lineage-directed .Abstract.

The group of biologically active nitroheterocyclic compounds includes various 5- and 2-nitroimidazoles and 5-nitrofurans, which can be used as therapeutic agents against a variety of protozoan and bacterial (anaerobic) infections of humans and animals.

Drug and Chemical Toxicology. Impact Factor. Search in: Advanced search In vivo genotoxicity assessment of sunset yellow and sodium benzoate in female rats. Mohamed Yassin Ali, Books; Keep up to date.

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