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New pentasubstituted pyrrole hybrid atorvastatin-quinoline derivatives with antiplasmodial activity.
Bioorg Med Chem Lett
; 26(8): 1881-4, 2016 Apr 15.
Artículo
en Inglés
| MEDLINE
| ID: mdl-26988303
RESUMEN
Cerebral malaria is caused by Plasmodium falciparum. Atorvastatin (AVA) is a pentasubstituted pyrrole, which has been tested as an adjuvant in the treatment of cerebral malaria. Herein, a new class of hybrids of AVA and aminoquinolines (primaquine and chloroquine derivatives) has been synthesized. The quinolinic moiety was connected to the pentasubstituted pyrrole from AVA by a linker group (CH2)n=2-4 units. The activity of the compounds increased with the size of the carbons chain. Compound with n=4 and 7-chloroquinolinyl has displayed better activity (IC50=0.40 µM) than chloroquine. The primaquine derivative showed IC50=1.41 µM, being less toxic and more active than primaquine.