Detail of "22994-85-0"

Reference

Reductive metabolism and activation of benznidazole

Reductive metabolism and activation of benznidazole. Masana, Monica; De Toranzo, Edith G. D.; Castro, Jose A. (Cent. Invest. Toxicol., Argent.). Biochem. Pharmacol., 33(7), 1041-5 (English) 1984. CODEN: BCPCA6. ISSN: 0006-2952. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacology) A study of the reductive metab. and activation of benznidazole (Bz)(I) [22994-85-0], demonstrated that rat liver microsomal and cytosolic fractions, but not mitochondria, exhibited Bz nitroreductase [9037-41-6] activity under anaerobic conditions in the presence of NADPH. Microsomal nitroreductase activity was enhanced by FAD and was inhibited totally by O and partially by CO. The liver cytosol fraction was able to reduce Bz nitrogroups in the presence of either N-methylnicotinamide or hypoxanthine as substrates. These enzyme activities were inhibited by menadione or allopurinol, resp. Under every exptl. condition leading to enzymic redn. of Bz nitrogroups and its inhibition or enhancement, reactive metabolites that bind covalently to proteins were also produced. This covalent binding was effectively prevented by reduced glutathione. Results suggest the participation of cytochrome P 450 [9035-51-2] and cytochrome c reductase [9023-03-4] in liver microsomal processes, as well as xanthine oxidase [9002-17-9] and aldehyde oxidase [9029-07-6] involvement in liver cytosolic Bz nitroredn. and activation, resulting in reactive metabolites that bind covalently to proteins. Possible pharmacol. and toxicol. implications of the described observations are discussed.

Ultraviolet spectrophotometric determination of benznidazole

Ultraviolet spectrophotometric determination of benznidazole. Nothenberg, Michael Simon (Fac. Cienc. Farm., Univ. Sao Paulo, Sao Paulo, Brazil). Rev. Farm. Bioquim. Univ. Sao Paulo, 19(2), 69-77 (Portuguese) 1983. CODEN: RFBUBI. ISSN: 0370-4726. DOCUMENT TYPE: Journal CA Section: 64 (Pharmaceutical Analysis) Benznidazole (I) [22994-85-0] was detd. using 2 variations of a previously reported UV spectrophotometric method. The variations consisted of detns. based on a calibration curve in MeOH and in 0.1N HCl at 314 and 324 nm, resp. For the method using MeOH, the mean recovery was 99.39% and the variation coeff. was 1.36%; for the method using 0.1N HCl, those values were 100.47 and 0.77%, resp. Both methods gave equally satisfactory results.