التفاصيل البيبلوغرافية
| العنوان: |
New pentasubstituted pyrrole hybrid atorvastatin–quinoline derivatives with antiplasmodial activity. |
| المؤلفون: |
Carvalho, Rita C.C.1,2, Martins, Wagner A.1, Silva, Tayara P.3, Kaiser, Carlos R.2, Bastos, Mônica M.1, Pinheiro, Luiz C.S.1, Krettli, Antoniana U.3, Boechat, Núbia1 boechat@far.fiocruz.br |
| المصدر: |
Bioorganic & Medicinal Chemistry Letters. Apr2016, Vol. 26 Issue 8, p1881-1884. 4p. |
| مصطلحات موضوعية: |
*CEREBRAL malaria, *QUINOLINE derivatives, *PYRROLE derivatives, *ATORVASTATIN, *IMMUNOLOGICAL adjuvants, *PRIMAQUINE, *INHIBITORY Concentration 50, *THERAPEUTICS |
| مستخلص: |
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 (CH 2 ) 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 (IC 50 = 0.40 μM) than chloroquine. The primaquine derivative showed IC 50 = 1.41 μM, being less toxic and more active than primaquine. [ABSTRACT FROM AUTHOR] |
| قاعدة البيانات: |
Academic Search Index |
