Detail of "5213-49-0"

Reference

Hypoxic radiosensitizers: prospects for effective compounds with fewer toxic side-effects

Hypoxic radiosensitizers: prospects for effective compounds with fewer toxic side-effects. Rupp, W. D.; Mroczkowski, Z.; Agrawal, K. C. (Dep. Ther. Radiol., Yale Univ. Sch. Med., New Haven, Conn., USA). Br. J. Cancer, Suppl., 37(3), 60-3 (English) 1978. CODEN: BJCSB5. ISSN: 0306-9443. DOCUMENT TYPE: Journal CA Section: 3 (Biochemical Interactions) Three nitroimidazole and 3 NPR (3-nitro-2-methyl(thiopyrrole) [61201-15-8] were tested for radiosensitizing activity in Escherichia coli and compared with misonidazole (II) [13551-87-6] for toxic side-effects on endpoints such as mutagenesis, cell killing, and inhibition of b-galactosidase synthesis. Although the 4 compds. tested were comparable or superior to II with respect to radiosensitizing activity, there were marked differences in their side-effects. KA 121 (I) [5213-49-0] was the most promising for further study, because it combines good radiosensitization with low mutagenicity and toxicity.

Nitroimidazolones

Nitroimidazolones. Synthesis of deaza analogs of 3-nitro-1,2,4-triazol-5-one. Marlin, John E.; Killpack, Michael O. (Frank J. Seiler Res. Lab.Several reagents such as 5213-49-0 is used here., U.S.A.F. Acad., CO 80840, USA). Heterocycles, 34(7), 1385-93 (English) 1992. CODEN: HTCYAM. ISSN: 0385-5414. DOCUMENT TYPE: Journal CA Section: 28 (Heterocyclic Compounds (More Than One Hetero Atom)) Analogs of 3-nitro-1,2,4-triazol-5-one have been synthesized. The strategy revolves around a new method for the synthesis of imidazolones, namely the addn.-elimination reaction of the sodium salt of trimethylsilylethanol with a (trimethylsilyl)ethoxymethyl-protected dinitroimidazole followed by the acid-catalyzed conversion to the desired nitroimidazole. Thus, 2,4-dinitroimidazole reacted with 2-(trimethylsilyl)ethoxymethyl chloride to give the N-silyl deriv. which reacted with Me3SiCH2CH2OH to give ethoxynitroimidazole I. I reacted with F3CCO2H to give 1,3-dihydro-4-nitro-2H-imidazol-2-one (II). The N-Me deriv. of II was prepd. in a similar manner starting from the N-methyldinitroimidazole. .