C. Luu-Duc

Synthesis of new 4-amino-2,6-diarylpyrimidine-5-carbonitriles

A facile synthesis of the title compounds 5a–e, from appropriate amidines and benzylidenemalononitriles, is described.

Synthesis of 15-(p-iodophenyl) pentadecanoic acid labelled with carbon-14

15-(p-Iodophenyl) pentadecanoic acid labelled with carbon-14 in the carboxyl group is obtained with good yields in five steps from [14C]NaCN, starting from 14-bromo 1-phenyl tetradecane 2. Specific radioactivity: 0.019 mCi/mg, 8.45 mCi/mmol; radiochemical yield: 74.6%.

Influence of the presence of a methyl group on the myocardial metabolism of 15-(paraiodophenyl)-3 methyl pentadecanoic acid (IMPPA)

The objective of the present study was to determine the mechanism of accumulation of myocardial activity following i.v. injection of 15-(paraiodophenyl)-3 methyl pentadecanoic acid (IMPPA). IMPPA and 15 phenyl-3 methyl pentadecanoic acid (MPPA) were labeled with 14C at position 1 and used to perfuse isolated rat hearts in a closed system. After 5 min of perfusion, IMPPA reached 2/3 of its value at 45 min. 14CO2 production was low. Most of the myocardial activity was in the form of free IMPPA. Analysis of IMPPA activation by CoA SH revealed that it was very strongly inhibited. The retention of myocardial activity is thus due to intracellular accumulation of free IMPPA following inhibition of activation. Comparison of results obtained with IMPPA and MPPA showed that the presence of iodine in the molecule accentuates the inhibition of activation.