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4-Aminoquinoline derivatives:Synthesis, in vitro and in vivo antiplasmodial activity against chloroquine-resistant parasites

4-Aminoquinoline derivatives:Synthesis, in vitro and in vivo antiplasmodial activity against chloroquine-resistant parasites

Authors :
Singh, Shailja
Agarwal, Drishti
Sharma, Kumkum
Sharma, Manish
Nielsen, Morten A
Alifrangis, Michael
Singh, Ashok K
Gupta, Rinkoo D
Awasthi, Satish K
Singh, Shailja
Agarwal, Drishti
Sharma, Kumkum
Sharma, Manish
Nielsen, Morten A
Alifrangis, Michael
Singh, Ashok K
Gupta, Rinkoo D
Awasthi, Satish K
Source :
Singh , S , Agarwal , D , Sharma , K , Sharma , M , Nielsen , M A , Alifrangis , M , Singh , A K , Gupta , R D & Awasthi , S K 2016 , ' 4-Aminoquinoline derivatives : Synthesis, in vitro and in vivo antiplasmodial activity against chloroquine-resistant parasites ' , European Journal of Medicinal Chemistry , vol. 122 , pp. 394-407 .
Publication Year :
2016

Abstract

Synthetic quinoline derivatives continue to be considered as candidates for new drug discovery if they act against CQ-resistant strains of malaria even after the widespread emergence of resistance to CQ. In this study, we explored the activities of two series of new 4-aminoquinoline derivatives and found them to be effective against Plasmodium falciparum under in vitro conditions. Further, we selected four most active derivatives 1m, 1o, 2c and 2j and evaluated their antimalarial potential against Plasmodium berghei in vivo. These 4-aminoquinolines cured BALB/c mice infected with P. berghei. The ED50 values were calculated to be 2.062, 2.231, 1.431, 1.623 and 1.18 mg/kg of body weight for each of the compounds 1m, 1o, 2c, 2j and amodiaquine, respectively. Total doses of 500 mg/kg of body weight were well received. The study suggests that these new 4-aminoquinolines should be used for structure activity relationship to find lead molecules for treating multidrug-resistant Plasmodium falciparum and Plasmodium vivax.

Details

Database :
OAIster
Journal :
Singh , S , Agarwal , D , Sharma , K , Sharma , M , Nielsen , M A , Alifrangis , M , Singh , A K , Gupta , R D & Awasthi , S K 2016 , ' 4-Aminoquinoline derivatives : Synthesis, in vitro and in vivo antiplasmodial activity against chloroquine-resistant parasites ' , European Journal of Medicinal Chemistry , vol. 122 , pp. 394-407 .
Notes :
English
Publication Type :
Electronic Resource
Accession number :
edsoai.on1322682406
Document Type :
Electronic Resource