The enzyme trypanothione reductase (TR) which restores the oxidized trypanothione to reduced state has evolved as an effective drug target. Many inhibitors of this enzyme have been developed but most of them combat with problems related to bioavailability, pharmacokinetics and metabolism. Despite this quinolines have evolved as most important class of compounds against TR due to their broad spectrum of activity, excellent pharmacological and pharmacokinetic properties such as high plasma levels, high clearance, oral and parenteral applicability, chemical stability and rare side effect.