title: BATO complexes derived from dimethoxy dioximes: synthesis, characterization and biodistribution.
abstract: To prepare less lipophilic BATO complexes, two new methoxy-substituted dioximes were synthesized: cis-4,5-dimethoxycyclohexane-1,2-dione dioxime (DMCDO) and 1,4-dimethoxybutane-2,3-dione dioxime (DMDMG). 99mTcCl(DMCDO)3BMe (BMe = methylboronic acid) was prepared and characterized. Reversed-phase HPLC analyses of 99mTcCl(DMCDO)3BMe and 99mTcCl(DMCDO)3-p-TBA (p-TBA = p - tolylboronic acid) indicated that both of these complexes were mixtures of four enantiomeric pairs of diastereomers. Attempted preparation of a BATO complex from DMDMG gave a mixture of products. In rats, 99mTcCl(DMCDO)3BMe displayed more rapid liver and renal clearance than 99mTcCl(CDO)3BMe, but 99mTcCl(DMCDO)3BMe and 99mTcCl(DMCDO)3-p-TBA displayed low uptake in both heart and brain.
authors.affiliation: Bristol-Myers Squibb Pharmaceutical Research Institute, Princeton, NJ 08543, USA.
authors.forename: K
authors.initials: K
authors.lastname: Ramalingam
authors.forename: S S
authors.initials: SS
authors.lastname: Jurisson
authors.forename: B L
authors.initials: BL
authors.lastname: Kuczynski
authors.forename: R
authors.initials: R
authors.lastname: Di Rocco
authors.forename: R K
authors.initials: RK
authors.lastname: Narra
authors.forename: D P
authors.initials: DP
authors.lastname: Nowotnik
authors.forename: A D
authors.initials: AD
authors.lastname: Nunn
mesh_terms: D000818:Animals; D002851:Chromatography, High Pressure Liquid; D015902:Gamma Cameras; D007553:Isotope Labeling; D008297:Male; D015609:Organotechnetium Compounds / Q000138:chemical synthesis / Q000737:chemistry; D010091:Oximes / Q000138:chemical synthesis / Q000737:chemistry; D051381:Rats; D013056:Spectrophotometry, Ultraviolet; D013237:Stereoisomerism; D014018:Tissue Distribution
chemical_list: D015609:Organotechnetium Compounds; D010091:Oximes