European Journal of Medicinal Chemistry p. 527 - 536 (2013)
Update date:2022-08-15
Topics: Synthesis Biological Evaluation Design antileishmanial agents
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
Gupta, Suman
Puri, Sunil K.
Launay, Delphine
Martin, Denis
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.
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