4-Aminoquinoline derivatives: Synthesis, in vitro and in vivo antiplasmodial activity against chloroquine-resistant parasites
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4-Aminoquinoline derivatives : Synthesis, in vitro and in vivo antiplasmodial activity against chloroquine-resistant parasites. / Singh, Shailja; Agarwal, Drishti; Sharma, Kumkum; Sharma, Manish; Nielsen, Morten A; Alifrangis, Michael; Singh, Ashok K; Gupta, Rinkoo D; Awasthi, Satish K.
In: European Journal of Medicinal Chemistry, Vol. 122, 21.10.2016, p. 394-407.Research output: Contribution to journal › Journal article › Research › peer-review
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TY - JOUR
T1 - 4-Aminoquinoline derivatives
T2 - Synthesis, in vitro and in vivo antiplasmodial activity against chloroquine-resistant parasites
AU - Singh, Shailja
AU - Agarwal, Drishti
AU - Sharma, Kumkum
AU - Sharma, Manish
AU - Nielsen, Morten A
AU - Alifrangis, Michael
AU - Singh, Ashok K
AU - Gupta, Rinkoo D
AU - Awasthi, Satish K
N1 - Copyright © 2016 Elsevier Masson SAS. All rights reserved.
PY - 2016/10/21
Y1 - 2016/10/21
N2 - 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.
AB - 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.
KW - Faculty of Health and Medical Sciences
KW - Antimalarial
KW - Amodiaquine
KW - Chloroquine
KW - 4-Aminoquinoline analogues
KW - Plasmodium falciparum
KW - Plasmodium berghei
U2 - 10.1016/j.ejmech.2016.06.033
DO - 10.1016/j.ejmech.2016.06.033
M3 - Journal article
C2 - 27394399
VL - 122
SP - 394
EP - 407
JO - European Journal of Medicinal Chemistry
JF - European Journal of Medicinal Chemistry
SN - 0223-5234
ER -
ID: 163764105