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Judul: Senyawa Baru Potensialantimalaria Turunan 5-Bromo-1, 10-Fenantrolin: Sintesis Dan Uji Aktivitas
Penulis: Ruslin Hadanu  || email: info@mx.unpatti.ac.id
Jurnal: Molucca Medica Vol. 2 no. 1 - hal. 39-46 Tahun 2009  [ Kedokteran ]
Keywords:  1,10-phenanthroline, 5-bromo-1,10-phenanthroline derivatives, antimalarial activity
Abstract: The synthesis of 5-bromo-1, 10-phenanthroline derivatives with 1,10-phenanthroline monohydrate as starting material through two steps has been carried out. The first step of reaction is bromination of 1,10-phenanthroline using Br, and oleum was conducted by reflux for 8 h. The result of reaction is 5-bromo-1, 10-phenanthroline (74,11%) in the form of nutbrown solid. The second step of reaction is methylation and ethylation of 5-bromo-1, 10-phenathroline using DMS and DES reagents that its was refluxed for 7 and 8 h, respectively. The result of reaction are 6-bromo-(1)-N-methyl-1, 10phenanthrolinium sulfate and 6-bromo-(1)-N-ethyl-1, 10-phenanthrolinium sulfate in yield from 94,2 and 86,38%, respectively. The results of testing in vitro antiplasmodial activity at chloroquine-resistant P. falciparum FCR3 strain to 5-bromo-1, 10-phenanthroline derivatives obtained that 6-bromo-(1)-N-methyl-1, 10-phenanthrolinium sulfate has higher antimalarial activity (IC50 – 0,06 ±0,4 µM) than antimalarial activity of 5-bromo-1, 10-phenantroline (IC50 = 1,66 ±0,77 µM) and 6-bromo-(1)-N-methyl-1, 10- phenanthrolinium sulfate (IC50= 0,22±0,18 µM). while, the results of reaction are 6-bromo-(1)-N-methyl-1, 10-phenanthrolinium sulfate and 6-bromo-(1)-N-methy-1,10-phenanthrolinium sulfate in yield from 94,2 and 86,38%, respectively. The results of testing in in vitro antiplasmodial activity at chloroquine-resistant P. falciparum D10 strain to 5-bromo-1, 10-phenanthroline derivatives obtained that 6-bromo-(1)-N-methyl-1, 10-phenanthrolinium sulfate has higher antimalarial activity (IC50=0,03±0,01 µM) than antimalarial activity of 5-bromo-1, 10-phenanthroline (IC50=1.13±0,070 µM) and 6-bromo-(1)-N-methyl1, 10-phenanthrolinium sulfate (IC50=0,41±0,01 µM).
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