background: cutaneous leishmaniasis (cl) is endemic in many tropical and subtropical regions of the world. due to the prolonged duration of therapy, adverse effect and resistance to current drugs in the treatment of cl, the dis­covery of novel, efficient, and safe leishmanicidal drugs is required. the aims of the present study was to synthesis of new compounds based on the active compounds of 5...

Reductive metabolism of the aromatic nitro group of 5-nitrofurans is thought to be an important step in the mechanism of their toxicity. Microsomal nitroreductase activity with p-nitrobenzoic acid and N-[4-(5-nitro-2-furyl)-2-thiazolyl[formamide (FANFT) as substrates was assessed in the renal cortex, outer medulla, inner medulla, bladder transitional epithelial and non-epithelial bladder tissue...

A series of nitrofuran-based compounds were identified as inhibitors of estrogen signaling in a cell-based, high-throughput screen of a diverse library of small molecules. These highly related compounds were subsequently found to inhibit topoisomerase II in vitro at concentrations similar to that required for the inhibition of estrogen signaling in cells. The most potent nitrofuran discovered i...

5-Nitrofurans have been used in the study of chemical carcinogenesis. There is substantial evidence that N-[4-(5-nitro-2-furyl)-2-thiazolyl] formamide (FANFT) is deformylated to 2-amino-4-(5-nitro-2-furyl)thiazole (ANFT) in the process of FANFT-induced bladder cancer. Paradoxically, ANFT is less potent as a uroepithelial carcinogen than FANFT when fed to rats. Feeding aspirin with FANFT to rats...

Nitrofurantoin is a synthetic nitrofuran compound. It is generally used in urinary tract infections, either alone or in combination with other antibiotics. A number of adverse effects may develop in different body systems during nitrofurantoin treatment; however, concomitant pulmonary and hepatotoxicity are rare. In this paper, we present a case of acute respiratory distress syndrome and hepato...

The carcinogenicity of N-( 5-Nitro-2-furfurylidene )-1-aminohydan to in (nitrofurantoin, NF-153) was examined in (C57BL/6N x DBA/2N)F1 (BDF1) mice. Three hundred of mice were divided into three groups, each group consisting about 50 male and 50 female mice. Nitrofurantoin was given in powdered diet at dose levels of 0. 3, 0. 075, or 0 % to the respestive group of mice. The overall incidence of ...

Nitrofurazone is one of the antibacterial nitrofuran agents used topically for skin infections. The drug is effective on the majority of infectious microorganisms. Because of the importance of this drug in clinic, in this study various methods of synthesis of nitrofurazone were examined and the most appropriate method, applicable to pharmaceutical industry was chosen and optimized from the poin...

A direct and facile synthesis of highly functional 5-aza-spiro[2,4]heptanes, a valuable structural motif for drug discovery, is developed via catalytic asymmetric 1,3-dipolar cycloaddition of cyclopropylidene acetate and azomethine ylides for the first time.

A novel synthesis of 1,2-disubstituted 1,2-dihydroquinazoline 3-oxides 8 and the first ever examples of 1,3-dipolar trapping of these nitrones to homonuclear dipolarophiles is described. The new dipoles 8 reacted with N-methyl maleimide, generating diastereomeric adducts 14-16. In the reaction between 8 and dimethyl acetylenedicarboxylate, primary cycloadducts 17 and/or stable rearrangement pro...