-transparent.png){kind=logo}
Design, synthesis and biological evaluation of 2-substituted quinolines as potential antileishmanial agents. 2013
Vadiraj S Gopinath, and
Jakir Pinjari, and
Ravindra T Dere, and
Aditya Verma, and
Preeti Vishwakarma, and
Rahul Shivahare, and
Manjunath Moger, and
Palusa Sanath Kumar Goud, and
Vikram Ramanathan, and
Prosenjit Bose, and
M V S Rao, and
Suman Gupta, and
Sunil K Puri, and
Delphine Launay, and
Denis Martin
Advinus Therapeutics Pvt. Ltd., Bangalore 560 058, India.
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.
Related Publications
Vadiraj S Gopinath, and
Jakir Pinjari, and
Ravindra T Dere, and
Aditya Verma, and
Preeti Vishwakarma, and
Rahul Shivahare, and
Manjunath Moger, and
Palusa Sanath Kumar Goud, and
Vikram Ramanathan, and
Prosenjit Bose, and
M V S Rao, and
Suman Gupta, and
Sunil K Puri, and
Delphine Launay, and
Denis Martin
September 2022,
Bioorganic & medicinal chemistry letters,
Vadiraj S Gopinath, and
Jakir Pinjari, and
Ravindra T Dere, and
Aditya Verma, and
Preeti Vishwakarma, and
Rahul Shivahare, and
Manjunath Moger, and
Palusa Sanath Kumar Goud, and
Vikram Ramanathan, and
Prosenjit Bose, and
M V S Rao, and
Suman Gupta, and
Sunil K Puri, and
Delphine Launay, and
Denis Martin
April 2022,
Molecules (Basel, Switzerland),
Vadiraj S Gopinath, and
Jakir Pinjari, and
Ravindra T Dere, and
Aditya Verma, and
Preeti Vishwakarma, and
Rahul Shivahare, and
Manjunath Moger, and
Palusa Sanath Kumar Goud, and
Vikram Ramanathan, and
Prosenjit Bose, and
M V S Rao, and
Suman Gupta, and
Sunil K Puri, and
Delphine Launay, and
Denis Martin
June 2014,
European journal of medicinal chemistry,
Vadiraj S Gopinath, and
Jakir Pinjari, and
Ravindra T Dere, and
Aditya Verma, and
Preeti Vishwakarma, and
Rahul Shivahare, and
Manjunath Moger, and
Palusa Sanath Kumar Goud, and
Vikram Ramanathan, and
Prosenjit Bose, and
M V S Rao, and
Suman Gupta, and
Sunil K Puri, and
Delphine Launay, and
Denis Martin
May 2018,
European journal of medicinal chemistry,
Vadiraj S Gopinath, and
Jakir Pinjari, and
Ravindra T Dere, and
Aditya Verma, and
Preeti Vishwakarma, and
Rahul Shivahare, and
Manjunath Moger, and
Palusa Sanath Kumar Goud, and
Vikram Ramanathan, and
Prosenjit Bose, and
M V S Rao, and
Suman Gupta, and
Sunil K Puri, and
Delphine Launay, and
Denis Martin
March 2022,
Pakistan journal of pharmaceutical sciences,
Vadiraj S Gopinath, and
Jakir Pinjari, and
Ravindra T Dere, and
Aditya Verma, and
Preeti Vishwakarma, and
Rahul Shivahare, and
Manjunath Moger, and
Palusa Sanath Kumar Goud, and
Vikram Ramanathan, and
Prosenjit Bose, and
M V S Rao, and
Suman Gupta, and
Sunil K Puri, and
Delphine Launay, and
Denis Martin
August 2007,
Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie,
Vadiraj S Gopinath, and
Jakir Pinjari, and
Ravindra T Dere, and
Aditya Verma, and
Preeti Vishwakarma, and
Rahul Shivahare, and
Manjunath Moger, and
Palusa Sanath Kumar Goud, and
Vikram Ramanathan, and
Prosenjit Bose, and
M V S Rao, and
Suman Gupta, and
Sunil K Puri, and
Delphine Launay, and
Denis Martin
September 2009,
Bioorganic & medicinal chemistry letters,
Vadiraj S Gopinath, and
Jakir Pinjari, and
Ravindra T Dere, and
Aditya Verma, and
Preeti Vishwakarma, and
Rahul Shivahare, and
Manjunath Moger, and
Palusa Sanath Kumar Goud, and
Vikram Ramanathan, and
Prosenjit Bose, and
M V S Rao, and
Suman Gupta, and
Sunil K Puri, and
Delphine Launay, and
Denis Martin
January 2018,
Current computer-aided drug design,
Vadiraj S Gopinath, and
Jakir Pinjari, and
Ravindra T Dere, and
Aditya Verma, and
Preeti Vishwakarma, and
Rahul Shivahare, and
Manjunath Moger, and
Palusa Sanath Kumar Goud, and
Vikram Ramanathan, and
Prosenjit Bose, and
M V S Rao, and
Suman Gupta, and
Sunil K Puri, and
Delphine Launay, and
Denis Martin
January 2020,
Bioorganic & medicinal chemistry,
Vadiraj S Gopinath, and
Jakir Pinjari, and
Ravindra T Dere, and
Aditya Verma, and
Preeti Vishwakarma, and
Rahul Shivahare, and
Manjunath Moger, and
Palusa Sanath Kumar Goud, and
Vikram Ramanathan, and
Prosenjit Bose, and
M V S Rao, and
Suman Gupta, and
Sunil K Puri, and
Delphine Launay, and
Denis Martin
June 2022,
Future medicinal chemistry,
