Nitrazepam is metabolized in part by nitro-reduction to an amine followed by acetylation. This acetylation step has been shown to be under the control of the same genetic polymorphism as sulphamethazine (syn: sulphadimidine).

The biotransformation of A/-[4-(5-nitro-2-furyl)-2-thiazolyl]formamide (FANFT), a potent urinary bladder carcinogen, was studied in mice. About 82% of radioactivity was excreted as 14C02within 36 hr after intragastric administration of /V-[4-(5-nitro-2-furyl)-2thiazolyl]-[14C]formamide, suggesting its deformylation to 2amino-4-(5-nitro-2-furyl)thiazole (ANFT). The latter was formed in vitro as ...

Solubility and permeability of nitrofurantoin (NITRO) were compared with those its cocrystals containing isoniazid (ISO), bipyridyl (BIP), or phenanthroline (PHE) as coformers, their parent mixtures. NITRO dissolution profiles evaluated via HPLC; we resorted to molecular dynamics (MD) simulations rationalize the experimental data on basis nitrofurantoin–coformers nitrofurantoin–water intermolec...

Inactivation of the human DNA repair protein, O6-alkylguanine-DNA-alkyltransferase (AGT), by exposure to O6-benzylguanine leads to a dramatic enhancement in the cytotoxic response of cells to chemotherapeutic alkylnitrosoureas. Benzylated pyrimidines identified as more potent inactivators than O6-benzylguanine in vitro include 2,4-diamino-6-benzyloxy-5-nitrosopyrimidine (5-nitroso-BP) and 2,4-d...