Synthesis and antimalarial evaluation of novel pyridine quinoline hybrids |
| |
Authors: | Badri Narayan Acharya D Thavaselvam Mahabir Parshad Kaushik |
| |
Institution: | (1) Defence Research and Development Establishment, Discovery Center, Jhansi Road, Gwalior, 474002, M.P, India;(2) Defence Research and Development Establishment, Division of Microbiology, Jhansi Road, Gwalior, 474002, M.P, India |
| |
Abstract: | Abstract Synthesis and evaluation of the antimalarial activity of new pyridine quinoline hybrid molecules against a chloroquine-susceptible
strain of Plasmodium falciparum and as inhibitors of β-hematin formation are described. Two novel pyridine quinoline hybrid molecules and one bisquinoline
molecule were synthesized and purified by column chromatography and evaluated for antimalarial and haem polymerization inhibition
(HPIA) activities. The molecules were found to be very good haem polymerization inhibitors but showed poor antimalarial activity.
This was attributed to their low vacuole accumulation ratio (VAR) in comparison to chloroquine. These molecules can be used
as templates for designing new antimalarials targeting haem detoxification pathway of malaria parasite.
Graphical Abstract
Synthesis and antimalarial evaluation of novel pyridine quinoline hybrids
B.N Acharya, D. Thavaselvam# and M.P Kaushik*
Discovery Centre, Process Technology Development Division
Defence R & D Establishment, Jhansi Road, Gwalior-474002 (MP) INDIA
#Division of Microbiology, Defence Research and Development Establishment,Gwalior-474002, India
Synthesis and evaluation of antimalarial activity of new pyridine–quinoline hybrid molecules against a chloroquine-susceptible
strain of Plasmodium falciparum and as inhibitors of β-hematin formation are described. |
| |
Keywords: | Malaria P falciparum Haem detoxification Hematin Pyridine– quinoline hybrid molecules |
本文献已被 SpringerLink 等数据库收录! |
|