Pharmacological disposition and metabolic fate of 2′-fluoro-5-iodo-1-β-D-arabinofuranosylcytosine in mice and rats was written by Chou, Ting-Chao; Feinberg, Aaron; Grant, Alan J.; Vidal, Pedro; Reichman, Uri; Watanabe, Kyoichi A.; Fox, Jack J.; Philips, Frederick S.. And the article was included in Cancer Research on September 30,1981.Name: 4-Amino-1-((2R,3S,4R,5R)-3-fluoro-4-hydroxy-5-(hydroxymethyl)tetrahydrofuran-2-yl)pyrimidin-2(1H)-one The following contents are mentioned in the article:
2′-Fluoro-5-iodo-1-β-D-arabinofuranosylcytosine-HCl (FIAC)(I) [69123-90-6] was synthesized and labeled with 14C in the 2 position for the study of pharmacol. disposition and metabolic fate. FIAC is deaminated by cytosine nucleoside deaminase [9025-06-3] at a rate comparable to that of 1-β-D-arabinofuranosylcytosine. The deaminated product, 2′-fluoro-5-iodo-1-β-D-arabinofuranosyluracil (FIAU) [69123-98-4] is, like FIAC, an active antiviral agent. After i.v. injection of [2-14C]-FIAC in mice, most of the radioactivity in plasma appears as FIAU. In i.v.-injected rats which lack cytosine nucleoside deaminase, plasma radioactivity is largely present in unchanged FIAC. If mice are pretreated with tetrahydrouridine, an inhibitor of the nucleoside deaminase, plasma radioactivity is mostly FIAC. The radioactivity of [2-14C]-FIAC injected i.v. is excreted in urine, at 63 to 93% of the dose in mice and >90% of the dose in rats within 0 to 24 h. Most of the radioactivity in urine of rats and in mice pretreated with tetrahydrouidine is present as unchanged FIAC; in control mice, most of the radioactivity is found as FIAU. Chromatog. anal. of urine from control mice receiving labeled FIAC has revealed that radioactivity is present in the following nucleosides: FIAC (14.5); FIAU (73); 2′-fluoro-5-methyl-1-β-D-arabinofuranosyluracil (FMAU) [69256-17-3] (5.4); and 2′-fluoro-1-β-D-arabinofuranosyluracil [69123-94-0] (2.3%). These metabolites are also present in acid-soluble fractions of mouse blood, small intestine, and liver. Like FIAC and FIAU, FMAU is a potent antiherpetic agent. Only â?.3% of the radioactivity of injected [2-14C]-FIAC appears in mouse respiratory CO2; degradation to CO2 can be blocked by tetrahydrouridine. Less than 2% of the total radioactivity is excreted in bile in rats. Small amounts of radioactivity are also recovered in feces, mostly in deaminated products. FIAC and FIAU, with a 2′-F substituent in the arabino configuration, are less susceptible to metabolic glycosyl cleavage than is 5-iodo-2′-deoxyuridine. The radioactivity of [2-14C]-FIAC is incorporated into DNA fractions of highly proliferating organs such as intestine, spleen, and thymus, although preliminary results indicate that the substances incorporated are arabinofuranosyl nucleoside metabolites of FIAC. This study involved multiple reactions and reactants, such as 4-Amino-1-((2R,3S,4R,5R)-3-fluoro-4-hydroxy-5-(hydroxymethyl)tetrahydrofuran-2-yl)pyrimidin-2(1H)-one (cas: 56632-83-8Name: 4-Amino-1-((2R,3S,4R,5R)-3-fluoro-4-hydroxy-5-(hydroxymethyl)tetrahydrofuran-2-yl)pyrimidin-2(1H)-one).
4-Amino-1-((2R,3S,4R,5R)-3-fluoro-4-hydroxy-5-(hydroxymethyl)tetrahydrofuran-2-yl)pyrimidin-2(1H)-one (cas: 56632-83-8) belongs to pyrimidine derivatives. The aromatic compound pyrimidine, and its derivatives, are ubiquitous in nature. They are found in nucleic acids, vitamins, amino acids, antibiotics, alkaloids, and a variety of toxins. Therapy for fungal infections is based mainly on four classes of antifungals: azoles, echinocandins, polyenes, and pyrimidine analogs.Name: 4-Amino-1-((2R,3S,4R,5R)-3-fluoro-4-hydroxy-5-(hydroxymethyl)tetrahydrofuran-2-yl)pyrimidin-2(1H)-one
56632-83-8;4-Amino-1-((2R,3S,4R,5R)-3-fluoro-4-hydroxy-5-(hydroxymethyl)tetrahydrofuran-2-yl)pyrimidin-2(1H)-one;The future of 56632-83-8;New trend of C9H12FN3O4;function of 56632-83-8