Synthesis and biodistribution of novel ^99mTc‐nitrido methylpiperidine dithioformate derivatives as potential brain imaging agents

Abstract

Three dithioformate ligands with methyl substituted on the piperidine rings, potassium 1-(2-methylpiperidine-1-yl)-dithioformate (2-mp), potassium 1-(3-methylpiperidine-1-yl)-dithioformate (3-mp) and potassium 1-(4-methylpiperidine-1-yl)-dithioformate (4-mp) were synthesized. The corresponding 99m Tc-nitrido complexes were prepared in high yield (495% TcN-4mp, demonstrated the best properties for brain imaging with the brain uptake 3.4070.24, 3.2270.31, 2.7270.28 and 2.2270.18% ID/g at 5, 30, 60 and 120 min p.i., respectively. Moreover, the influence of stereochemistry of the 99m TcN complexes with methyl substitution on ortho, meta and para positions on piperidine ring on the biodistribution properties were investigated with B3LYP/6-31G*(LANL2DZ for Tc) method using the Gaussian 03 program package.

Preparation and Evaluation of Novel Folate Isonitrile 99mTc Complexes as Potential Tumor Imaging Agents to Target Folate Receptors

“…99m Tc is the most widely used SPECT radionuclide with good nuclide properties, including a half-life of 6.02 h, emission of 140 keV γ-rays, and the advantages of coordinated chemical diversity. Therefore, 99m Tc complexes are often used in the clinical diagnosis of some diseases, accounting for more than 85% of nuclear medicine SPECT images [ 8 , 9 ]. Recently, a number of 99m Tc-labeled folate-based conjugates have been developed as potential folate receptor imaging agents [ 10 , 11 , 12 , 13 , 14 ].…”

Synthesis, spectral characterization, DFT studies and biological activity of novel Ligand 1‐(2‐cyclohexyl thioethyl) piperidine and its complexes with group 12 metal chlorides

“…Ruthenium‐carbonyl‐piperidine complexes catalyze the oxidation of cinnamaldehyde and show antibacterial and antifungal activity . 99m Tc‐nitrido dithioformate complexes containing piperidine rings can act as brain imaging agents . Various aspects of allyl amination of Pd (II) allyl complexes containing chelating chalcogenated pyridine derivatives have been studied …”

Preparation and biological evaluation of 99mTcN‐labeled pteroyl‐lys derivative as a potential folate receptor imaging agent

“…Among them, 111 In‐DTPA‐folate ( γ ) has been evaluated in phase I/II clinical studies and appeared to be an effective probe to distinguish benign and malignant ovarian masses . Compared with 111 In, 99m Tc is the most widely used radionuclide in routine nuclear medicine because of its almost ideal physical decay properties (T 1/2 = 6.02 h, E γ = 140 Kev) and the availability through commercial 99 Mo/ 99m Tc generator . The development of new 99m Tc‐based FR imaging agents with optimal characteristics has been a subject of interest in the radiopharmaceutical field.…”