Novel Hydrazone derivatives of N-Amino-11-Azaartemisinin with High Order of Antimalarial Activity against Multidrug-Resistant Plasmodium yoelii nigeriensis in Swiss Mice via intramuscular route

Author(s):  
Manvika Karnatak ◽  
Mohammad Hassam ◽  
Ajit Shankar Singh ◽  
Dinesh Kumar Yadav ◽  
Chandan Singh ◽  
...  
2012 ◽  
Vol 56 (7) ◽  
pp. 3475-3480 ◽  
Author(s):  
Sovitj Pou ◽  
Rolf W. Winter ◽  
Aaron Nilsen ◽  
Jane Xu Kelly ◽  
Yuexin Li ◽  
...  

ABSTRACTSontochin was the original chloroquine replacement drug, arising from research by Hans Andersag 2 years after chloroquine (known as “resochin” at the time) had been shelved due to the mistaken perception that it was too toxic for human use. We were surprised to find that sontochin, i.e., 3-methyl-chloroquine, retains significant activity against chloroquine-resistant strains ofPlasmodium falciparum in vitro. We prepared derivatives of sontochin, “pharmachins,” with alkyl or aryl substituents at the 3 position and with alterations to the 4-position side chain to enhance activity against drug-resistant strains. Modified with an aryl substituent in the 3 position of the 7-chloro-quinoline ring, Pharmachin 203 (PH-203) exhibits low-nanomolar 50% inhibitory concentrations (IC50s) against drug-sensitive and multidrug-resistant strains andin vivoefficacy against patent infections ofPlasmodium yoeliiin mice that is superior to chloroquine. Our findings suggest that novel 3-position aryl pharmachin derivatives have the potential for use in treating drug resistant malaria.


2000 ◽  
Vol 94 (3) ◽  
pp. 190-193 ◽  
Author(s):  
Renu Tripathi ◽  
Aseem Umesh ◽  
Meenu Mishra ◽  
S.K. Puri ◽  
G.P. Dutta

RSC Advances ◽  
2016 ◽  
Vol 6 (28) ◽  
pp. 23718-23725 ◽  
Author(s):  
Lalit Yadav ◽  
Mohit K. Tiwari ◽  
Bharti Rajesh Kumar Shyamlal ◽  
Manas Mathur ◽  
Ajit K. Swami ◽  
...  

Bicyclic and tricyclic aza-peroxides were synthesized and assessed for theirin vitroandin vivoantimalarial activities againstPlasmodium falciparum(3D7 strain) andPlasmodium yoelii nigeriensisin Swiss mice by an oral route, respectively.


2010 ◽  
Vol 20 (15) ◽  
pp. 4459-4463 ◽  
Author(s):  
Chandan Singh ◽  
Ved Prakash Verma ◽  
Niraj Krishna Naikade ◽  
Ajit Shankar Singh ◽  
Mohammad Hassam ◽  
...  

1997 ◽  
Vol 17 (7) ◽  
pp. 419-423 ◽  
Author(s):  
A AWASTHI ◽  
S. MEHROTRA ◽  
V. BHAKUNI ◽  
G.P. DUTTA ◽  
H.B. LEVY ◽  
...  

2013 ◽  
Vol 10 (8) ◽  
pp. 741-747 ◽  
Author(s):  
Roberta Soares ◽  
Roberta Corrales ◽  
Fernanda Lopes ◽  
Marcio Alves ◽  
Adilson Silva ◽  
...  

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