China
Africa
Explore chapters and articles related to this topic
Organic Chemicals
Published in William J. Rea, Kalpana D. Patel, Reversibility of Chronic Disease and Hypersensitivity, Volume 4, 2017
William J. Rea, Kalpana D. Patel
Nitrofurans and nitroheterocyclics are drugs and potent carcinogens. Many nitrofurans have been synthesized for drugs with antibacterial activity. These are not only used particularly in veterinary practice but also in humans.
Furazolidone (Furazolidine)
Published in M. Lindsay Grayson, Sara E. Cosgrove, Suzanne M. Crowe, M. Lindsay Grayson, William Hope, James S. McCarthy, John Mills, Johan W. Mouton, David L. Paterson, Kucers’ The Use of Antibiotics, 2017
Furazolidine (also called furazolidone) is a synthetic nitrofuran derivative with broad-spectrum antiprotozoal and antibacterial activity. It is closely related to nitrofurantoin (see Chapter 97, Nitrofurans: Nitrofurazone, Furazidine, and Nitrofurantoin), an antibiotic used principally for the treatment of urinary tract infections (Chamberlain, 1976; Goodman et al., 1985).
Hypoxia-activated prodrug derivatives of anti-cancer drugs: a patent review 2006 – 2021
Published in Expert Opinion on Therapeutic Patents, 2022
Emilie Anduran, Ludwig J Dubois, Philippe Lambin, Jean-Yves Winum
In 2019, the University of Nankai reported in patent CN110437281A isophosphoramide HAP prodrugs having nitro-containing aromatic heterocycles as reductase hypoxia responders and a pyridinium-modified alkylating nitrogen mustard. Some representative molecules 22–26, depicted in Figure 13, showed good tumor hypoxia response characteristics in vitro on different cell lines: mouse lung cancer 3LL tumor cells, PC-3 human prostate cancer cells, HepG2 human liver cancer cells, and B16 mouse melanoma cells. Hypoxia responsiveness of compounds 22-26 showed enhanced toxic effects when exposing cells to low oxygen concentration consistent with the release of the cytotoxic alkylating drug under hypoxia. In vivo assays on a mouse lung cancer 3LL tumor model showed that nitrofuran derivatives exhibited the best results on the tumor growth inhibition [70].
What are the immunopharmacological effects of furazolidone? A systematic review
Published in Immunopharmacology and Immunotoxicology, 2021
Ivan Brito Feitosa, Bruno Mori, Ana Paula de Azevedo dos Santos, Janaína Cecília Oliveira Villanova, Carolina Bioni Garcia Teles, Allyson Guimarães Costa
Nonetheless, furazolidone’s metabolism and cytotoxic mechanisms may vary between different types of cells with different metabolic capacities, and its cytotoxicity is not attributed to a single toxic intermediate [7,8]. Its activity spectra are related to the reducing potential of its 5-nitro group, which is between 250 and 270 mV. Nitroreduction, on the other hand, occurs through type I or II reduction of the nitro group in the presence of parasitic NADPH-cytochrome P450 reductases. Under anaerobic conditions, type I NTRs catalyze the reduction of nitrofurans (NFs) to produce anti-pathogenic hydroxylamine. Under aerobic conditions, nitroreduction, catalyzed by type II NTRs, produces reactive oxygen and nitrogen species (ROS/RNS), causing oxidative stress to pathogens and ultimately death [9].
An evaluation of nifurtimox for Chagas disease in children
Published in Expert Opinion on Orphan Drugs, 2021
Fernanda Lascano, Jaime Altcheh
NFX is a nitrofuran antiprotozoal drug effective against T. cruzi that is currently undergoing extensive new development efforts, seeking approval in endemic countries. It was manufactured by Bayer as Lampit©, and in the United States (US) FDA has recently approved a pediatric formulation that consists of dividable tablets in dose strengths of 30 and 120 mg that are specially formulated to be dispersed in water. This can aid in the dosing and administration of the drug to pediatric patients and allows increments of 15 mg to accommodate body weight adjusted dosing. The dosage indication is 10–20 mg/kg/day for patients weighing <40 kg and 8–10 mg/kg/day for patients weighing ≥40 kg. The daily dose is divided in three doses for all ages. Typically, this dosing regimen used to be maintained for at least 60–90 days, being the 60-day scheme the one approved in the US. Recently, a tendency to reduce treatment duration in CD was observed [36,37]. A phase 3 clinical trial of NFX compared 30 versus 60 days regimens showing no difference in parasitological treatment response at 1-year follow-up, suggesting that a 30-day duration regime is effective for parasite clearence mainly in infants. [23] A long-term follow-up of is under development to confirm the serological response to 60-day treatment and further evaluate all results on enrolled children (NCT02625974).