Iron overload disorder and diseases where iron mismanagement plays a crucial role require
orally available iron chelators with favourable pharmacokinetic and toxicity profile. Desferrithiocin
(DFT), a tridentate and orally available iron chelator has a favourable pharmacokinetic profile but its
use has been clinically restricted due to its nephrotoxic potential. The chemical architecture of the
DFT has been naturally well optimized for better iron chelation and iron clearance from human biological
system. Equally they are also responsible for its toxicity. Hence, subsequent research has been devoted
to develop a non-nephrotoxic analogue of DFT without losing its iron clearance ability.
The review has been designed to classify the compounds reported till date and to discuss the structure
activity relationship with reference to modifications attempted at different positions over pyridine and
thiazoline ring of DFT. Compounds are clustered under two major classes: (i) Pyridine analogues and
(ii) phenyl analogues and further each class has been further subdivided based on the presence or absence
and the number of hydroxy functional groups present over pyridine or phenyl ring of the DFT
analogues. Finally a summary and few insights into the development of newer analogues are provided.