Synthesis and biological evaluation of tricarbonyl Re(I) and Tc(I) complexes anchored by poly(azolyl)borates: application on the design of radiopharmaceuticals for the targeting of 5-HT1A receptors

Synthesis and biological evaluation of tricarbonyl Re(I) and Tc(I) complexes anchored by poly(azolyl)borates: application on the design of radiopharmaceuticals for the targeting of 5-HT1A receptors

Garcia, R.; Gano, L.; Maria, L.; Paulo, A.; Santos, I.; Spies, H.

The building blocks fac-99mTc{kappa3-HB(timMe)3}(CO)3] and fac-[99mTc{kappa3-R(mu-H)B(timMe)2}(CO)3] [R is H (4a), Ph (5a); timMe is 2-mercapto-1-methylimidazolyl] were obtained almost quantitatively by reacting fac-[99mTc(CO)3(H2O)3]+ with the corresponding scorpionate. These compounds cross the intact blood-brain barrier in mice, with significant retention in the case of 4a and 5a. Using 4a as the lead structure, we have synthesized the functionalized complexes fac-[M{kappa3-H(mu-H)B(timBu-pip)2}(CO)3] [M is Re (8), 99mTc (8a); timBu-pip is methyl[4-((2-methoxyphenyl)-1-piperazinyl)butyl, but suffer from a relatively fast washout.

Keywords: Technetium; Rhenium; Poly(azolyl)borates; 5HT1A receptor; Bivalent approach

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