Abstract
Three new metabolites of budralazine, an antihypertensive drug, were isolated from urine, bile and liver-perfusion effluent of rats, and their structures were identified by direct comparison with authentic samples. A major urinary metabolite was identified as the mercapturic acid conjugate of mesityl oxide, namely, N-acetyl-S-(1, 1-dimethyl-3-oxo)butyl-L-cysteine (M-14). A major biliary metabolite was identified as 1-[2-(1, 3-dimethyl-3-S-L-glutathionyl-butylidene)hydrazino]phthalazine(M-15). It was assumed that M-15 was derived from addition of glutathione to the terminal carbon-carbon double bond of budralazine. M-15 had two geometrical isomers with respect to the hydrazone linkage. Two isomers were clearly separated by HPLC. A major metabolite of liver-perfusion was confirmed as the carboxylic acid analogue of budralazine, namely, 4-(1-phthalazinyl)hydrazino-2-methyl-trans-2-pentenoic acid (M-16). M-16 was also found to be a major plasma metabolite.
Sign-in/Register to access full text options 
Talk to us
Join us for a 30 min session where you can share your feedback and ask us any queries you have
Schedule a callDisclaimer: All third-party content on this website/platform is and will remain the property of their respective owners and is provided on "as is" basis without any warranties, express or implied. Use of third-party content does not indicate any affiliation, sponsorship with or endorsement by them. Any references to third-party content is to identify the corresponding services and shall be considered fair use under The CopyrightLaw.
