Structure-activity relationship of 99mTc complexes of phenylenediamine-thiol-thioether ligands (PhAT) to brain uptake in rats

…, JM Kerr, JL Wu, LM Schultze, NE Salazar…

Index: McBride; Baldwin; Kerr; Wu; Schultze; Salazar; Chinitz; Byrne Journal of Medicinal Chemistry, 1993 , vol. 36, # 1 p. 81 - 86

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Citation Number: 17

Abstract

A novel class of ligands, phenylenediamine-thiol-thioether (PhAT), was synthesized, and their-Tc complexes were evaluated for potential use as a functional brain imaging agent. The ligands reacted with Na-TcOd and SnCl2 to form single, stable, neutral, and lipophilic- Tc complexes. Several of these complexes showed significant brain uptake and retention in rats. In particular, the S-ethyl, allyl, and propargyl derivatives had high initial brain uptake ( ...