Synthesis of oxalamide and triazine derivatives as a novel class of hybrid 4-aminoquinoline with potent antiplasmodial activity.
Frequency of malaria and its resistance to chemotherapeutic options are emerging rapidly. To counter this problem, a series of 4-aminoquinolines having oxalamide and triazine functionalities in the side chain were synthesized and screened for their antimalarial activities. Triazine derivative 48 found to be the most active against CQ sensitive strain 3D7 of Plasmodium falciparum in an in vitro assay with an IC(50) of 5.23 ng/mL and oxalamide derivative 13 showed an in vivo suppression of 70.45% on day 4 against CQ resistant strain N-67 of Plasmodium yoelii.
Sunduru
Naresh
N
Division of Medicinal and Process Chemistry, Central Drug Research Institute, Lucknow 226001, India.
Sharma
Moni
M
Srivastava
Kumkum
K
Rajakumar
S
S
Puri
S K
SK
Saxena
J K
JK
Chauhan
Prem M S
PM
D000577:Amides / Q000138:chemical synthesis* / Q000737:chemistry / Q000633:toxicity; D000634:Aminoquinolines / Q000138:chemical synthesis / Q000737:chemistry* / Q000633:toxicity; D000818:Animals; D000962:Antimalarials / Q000138:chemical synthesis* / Q000737:chemistry / Q000633:toxicity; D002522:Chlorocebus aethiops; D006420:Hemeproteins / Q000037:antagonists & inhibitors / Q000378:metabolism; D008297:Male; D051379:Mice; D010963:Plasmodium falciparum / Q000187:drug effects; D010967:Plasmodium yoelii / Q000187:drug effects; D014227:Triazines / Q000138:chemical synthesis* / Q000737:chemistry / Q000633:toxicity; D014709:Vero Cells
D000577:Amides; D000634:Aminoquinolines; D000962:Antimalarials; D006420:Hemeproteins; D014227:Triazines; C020753:hemozoin; C001920:4-aminoquinoline