European journal of medicinal chemistry · 2013
Design, synthesis and biological evaluation of 2-substituted quinolines as potential antileishmanial agents.
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Gopinath Vadiraj S, Pinjari Jakir, Dere Ravindra T, Verma Aditya, Vishwakarma Preeti, Shivahare Rahul, Moger Manjunath, Kumar Goud Palusa Sanath, Ramanathan Vikram, Bose Prosenjit, Rao M V S, Gupta Suman, Puri Sunil K, Launay Delphine, Martin Denis
Аннотация
An analogous library of 2-substituted quinoline compounds was synthesized with the aim to identify a potential drug candidate to treat visceral leishmaniasis. These molecules were tested for their in vitro and in vivo biological activity against Leishmania donovani. Metabolic stability of these compounds was also improved through the introduction of halogen substituents. Compound (26g), found to be the most active; exhibited an IC₅₀ value of 0.2 μM and >180 fold selectivity. The hydrochloride salt of (26g) showed 84.26 ± 4.44 percent inhibition at 50 mg/kg × 5 days (twice daily, oral route) dose in L. donovani/hamster model. The efficacy was well correlated with the PK data observed which indicating that the compound is well distributed.