Synthesis and biodistribution of six novel 99mTc complexes of 2-hydroxybenzaldehyde-amino acid Schiff bases.
For the purpose of developing novel diagnostic pharmaceuticals of 99mTc-labeled small-size complexes, six novel complexes of 99mTc-2-hydroxybenzaldehyde-amino acid Schiff bases were designed and synthesized, and their biodistributions in mice were investigated. All the compounds were obtained in radiochemical yields higher than 90% at optimal conditions, and poor uptakes in muscle, brain, heart and tumor were commonly observed with rapid blood clearance. Potentiality was revealed of good kidney imaging by 2-hydroxybenzaldehyde-alanine (L2) complex within 40 min post-injection. Good bone uptake of 2-hydroxybenzaldehyde-histidine (L4) and 2-hydroxybenzaldehyde-aspartic acid (L5) complexes, high spleen accumulation of 2-hydroxybenzaldehyde-glycine (L1) and 2-hydroxybenzaldehyde-cysteine (L3) complexes, and non-specific biodistribution of 2-hydroxybenzaldehyde-glutamic acid (L6) complex were demonstrated.
Wang
Mingzhao
M
Key Laboratory of Radiopharmaceuticals, Ministry of Education, Department of Chemistry, Beijing Normal University, People's Republic of China. wang-mzo@bnu.edu.cn
Meng
Zhaoxing
Z
Fu
Jisheng
J
D000596:Amino Acids / Q000737:chemistry*; D000818:Animals; D001547:Benzaldehydes / Q000737:chemistry*; D005260:Female; D006801:Humans; D051379:Mice; D008813:Mice, Inbred ICR; D019275:Radiopharmaceuticals / Q000138:chemical synthesis* / Q000493:pharmacokinetics; D012545:Schiff Bases / Q000737:chemistry / Q000493:pharmacokinetics; D017556:Technetium Compounds / Q000138:chemical synthesis* / Q000493:pharmacokinetics; D014018:Tissue Distribution
D000596:Amino Acids; D001547:Benzaldehydes; D019275:Radiopharmaceuticals; D012545:Schiff Bases; D017556:Technetium Compounds