Aqueous synthesis of derivatized cyclopentadienyl complexes of technetium and rhenium directed toward radiopharmaceutical application

Half-sandwich complexes of the type [(RCOCp)M(CO)(3)] with M = Re and (99(m))Tc were synthesized from [M(OH(2))(3)(CO)(3)](+) in water. The R group can be an organic residue or a receptor binding biomolecule with a spacer to cyclopentadienyl (Cp). This provides a general route to Cp complexes of technetium without the need for starting from [TcBr(CO)(5)]. The X-ray structure of [(C(6)H(5)CH(2)COC(5)H(4))Tc(CO)(3)] has been elucidated. The compound crystallizes in the monoclinic space group P2(1)/c with a = 16.1454(9), b = 7.6300(6), and c = 12.3922(7) A and beta = 107.792(6) degrees. We have chosen a serotonergic receptor ligand (WAY) as an example for the derivatization of Cp with a bioactive molecule. WAY is linked to Cp by an aliphatic chain of variable length. The half-sandwich complexes were prepared from water and organic solvents. The structure of [(WAY4-Cp)Re(CO)(3)] could be elucidated. The compound crystallizes in the monoclinic space group P2(1)/c with a = 15.7112(6), b = 6.8775(3), and c = 25.5217(12) A and beta = 103.778(5) degrees. Quantification of inhibition constants gave a clear structure-activity relationship. A single methylene group between the receptor binding site and the half-sandwich complex gave an IC(50) of 217 nM for HT(1A), whereas a butylene linker resulted in retention of the inhibition constant with an IC(50) of 6 nM with respect to underivatized WAY. For use as radiopharmaceuticals, the compounds have also been prepared with (99m)Tc in quantitative yield.     

Repeated Angles inE 4

Let there be givenn points in four-dimensional euclidean spaceE ₄. We show that the number of occurrences of the angle iso(n ³) if is not a right angle and (n ³) otherwise.     

Analysis of the phospholipid composition of plasmodium knowlesi and rhesus erythrocyte membranes

Methods for the separation and analysis of the phospholipid classes have been studied. The lipid extracts of normal and Plasmodium knowlesi- infected rhesus erythrocytes and of the parasite itself have been examined for phospholipid composition on an animal-to-animal basis. Several differences were apparent between the phospholipids of parasites and infected host cells. Phosphatidylinositol, phosphatidylcholine, and phosphatidylethanolamine represented larger percentages in the parasite than in the host; the average phosphatidylinositol content was 1.8 % in infected host cells and 4.3 % in parasites. Sphingomyelin and phosphatidylserine were also strikingly different in the two membranes; in the parasite they averaged less than 20 % and 33 % respectively of their level in the infected red blood cell.     

Empirical model of slow pyrolysis of hardwood chips

Applied Biochemistry and Biotechnology - The thermal decomposition of mixed hardwood chips was investigated by pyrolyzing 1-kg samples at atmospheric pressure in an electrically-heated batch...     

The boat-shaped polyketide resistoflavin results from re-facial central hydroxylation of the discoid metabolite resistomycin

Resistoflavin (1) is a rare boat-shaped pentacyclic polyketide metabolite of Streptomyces resistomycificus with marked antibacterial activity. By a series of experiments we have disclosed that the optically active molecule is derived from the discoid polyketide resistomycin (2) by an unusual, enantioface-differentiating hydroxylation, which leads to the capped pentacyclic ring system. In vivo and in vitro experiments unequivocally demonstrate that this reaction is catalyzed by RemO, an FAD-dependent monooxygenase. In addition, we were able to establish the absolute configuration of 1 and thus the stereochemical course of this rare enzymatic reaction by extensive computational methods. Comparison of the experimental CD spectrum with those quantum chemically calculated for (R)-1 and (S)-1 revealed the R-configuration of 1. Consequently, the enzyme-catalyzed hydroxylation takes place from the Re-face of 2 with loss of aromaticity in favor of a chiral carbinol center. While other oxygenases involved in polyketide tailoring functionalize the periphery of polyphenols, RemO is unique in its ability to catalyze a central, nonperipheral hydroxylation of a fused ring system.