Reference

Radioiodinated 1-(5-iodo-5-deoxy-b-D-arabinofuranosyl)-2-nitroimidazole (iodoazomycin arabinoside: IAZA): a novel marker of tissue hypoxia

Radioiodinated 1-(5-iodo-5-deoxy-b-D-arabinofuranosyl)-2-nitroimidazole (iodoazomycin arabinoside: IAZA): a novel marker of tissue hypoxia. Mannan, Rezaul H.; Somayaji, Vijayalakashmi V.; Lee, Jane; Mercer, John R.; Chapman, J. Donald; Wiebe, Leonard I. (Fac. Pharm. Pharm. Sci., Univ. Alberta, Edmonton, AB T6G 2N8, Can.). J. Nucl. Med., 32(9), 1764-70 (English) 1991. CODEN: JNMEAQ. ISSN: 0161-5505. DOCUMENT TYPE: Journal CA Section: 8 (Radiation Biochemistry) Section cross-reference(s): 14 1-(5-Iodo-5-deoxy-b-D-arabinofuranosyl)-2-nitroimidazole (IAZA) has been synthesized and labeled with 125I. Radioiodinated IAZA was shown to undergo hypoxia-dependent binding in EMT-6 cells in vitro and to have an initial binding rate of 284 pmole/106 cells/h at a substrate concn. of 30 mM. This binding rate is >3-fold that of the ref. compd., misonidazole (89 pmole/106 cells/h). The elevated binding rate was accompanied by in vitro cytotoxicity 30-40-fold greater than that obsd. for misonidazole. 527-73-1 and 83416-42-6 which are cas registry numbers of chemicals are mentioned. Whole-body elimination and biodistribution studies in BALB/c mice bearing implanted, s.c. EMT-6 tumors showed a rapid excretion (>98% in 24 h) with moderate tissue levels which, in general, declined as a function of blood clearance. Tumor-to-blood ratios of 4.6 (4 h) and 8.7 (8 h), with resp. tumor uptake values of 2.08% and 1.22% ID/g of tissue, form a rational basis for evaluation of this and related 2-nitroimidazole analogs as radiopharmaceuticals suitable for scintigraphic evaluation of tissue (tumor) hypoxia. .

Electrochemical reduction of 2-nitroimidazole in aprotic medium: Influence of its dissociation equilibrium on the reduction mechanism

All Rights Reserved. Electrochemical reduction of 2-nitroimidazole in aprotic medium: Influence of its dissociation equilibrium on the reduction mechanism. Squella, J. A.; Campero, A.; Maraver, J.; Carbajo, J. ( Bioelectrochemistry Laboratory, Chemical and Pharmaceutical Sciences Faculty, University of Chile, Olivos, Santiago 1007, Chile). 2052-49-5 and 527-73-1 are cas registry numbers. These chemicals are also mentioned in this article. Electrochimica Acta, 52(2), 511-518 (English) 2006 Elsevier B.V. CODEN: ELCAAV. ISSN: 0013-4686. DOCUMENT TYPE: Journal CA Section: 72 (Electrochemistry) Section cross-reference(s): 22, 68 The electrochem. redn. of 2-nitroimidazole in a nonaq. medium using cyclic voltammetry (CV) at a Hg electrode was carried out. The 2-nitroimidazole deriv. in DMF + 0.1M Bu4NPF6 resulted in the following dissocn. equil.: HNRNO2 t -NRNO2+H+. The neutral species (HNRNO2) and the corresponding conjugate base (-NRNO2) are characterized by UV absorption bands at 328 and 370 nm, resp. The voltammograms of 2-nitroimidazole produced 2 well-defined signals, which were detd. by the above dissocn. equil. The 1st redn. peak was caused by the redn. of the neutral species according to the following overall mechanism: 5HNRNO2 + 4e- t 4-NRNO2 + HNRNHOH + H2O. The 2nd quasi-reversible couple was caused by the redn. of the conjugate base according to the following equation:-NRNO2 + e- t NRNO2·-. .