Journal of Medicinal Chemistry p. 94 - 97 (1984)
Update date:2022-08-11
Topics:
Knapp, F. F.
Goodman, M. M.
Kabalka, G. W.
Sastry, K. A. R.
125I-labeled (E)-18-iodo-17-octadecenoic acid (13) has been prepared and evaluated in rats to determine the myocardial uptake and retention and degree of in vivo deiodination of this model iodovinyl-substituted fatty acid, which contains no structural perturbation to inhibit metabolism.This new agent was prepared by NaI-chloramine-T treatment of (17-carbomethoxyheptadec-1-en-1-yl)boronic acid (11) prepared by catecholborane treatment of methyl 17-octadecynoate (10), followed by basic hydrolysis to the free acid (13).The pivotal substrate, 17-octadecynoic acid (9), was prepared by two new routes .The 125I-labeled acid 13 showed high myocardial uptake (1 h, 1.90-2.28percent dose/g) with 45percent washout after 2 h but lower heart/blood ratios in comparison to analogues containing the tellurium heteroatom.Deiodination was low for the first 2 h after injection (2 h, 61percent dose/g).Excellent myocardial images were obtained in a dog with the 123I-labeled agent.
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