In Vitro Inhibition of β-Hematin by 2, 4-Diamino-6- Mercaptopyrimidine ＆ 2-Mercaptopyrimidine  

作　　者：Amneh Aljazzar Qasem Abu-Remeleh Abd-Alkareem Alsharif Mohammad Abul Haj Mutaz Akkawi 

机构地区：[1]Department of Life Sciences, College of Science and Technology, Al-Quds University 91999, Palestine [2]Department of Chemistry and Chemical Technology, College of Science and Technology, Al-Quds University 91999, Palestine

出　　处：《Journal of Chemistry and Chemical Engineering》2010年第12期57-61,共5页化学与化工（英文版）

摘　　要：Malaria is a disease that has drawn worldwide attention due to the alarming rise of mortality rates particularly in third world countries. During the Plasmodium parasite intraerythrocytic life cycle, metabolic processes include the formation of hemozoin or malaria pigment. This pigment functions in the prevention of oxygen radical-mediated damage to the parasite. Drugs targeting hemozoin formation such as chloroquine and amodaquine are effective and are still used, but recently Plasmodium parasites have become resistant to these drugs, especially against chloroquine. In this study we looked at the potential use of two heterocyclic pyrimidine derivatives as anti-malaria drugs; 2,4-Diamino-6-Mercaptopyrimidine （DAMP） and 2-Mercaptopyrimidine （2-MP）. These compounds bear various coordination sites that enable them to react with metal ions to form coordination compounds. We used two methods for testing the inhibition of ferriprotoporphyrin IX （FP） biomineralisation： semi-quantitative microassay used by Deharo, and a quantitative assay used by G. Blaner and M. Akkawi. We report here the finding that （DAMP） has an in vitro inhibitory effect on I%hematin formation at concentrations and magnitude of nearly similar order to that of chloroquine, 2-MP was found to be effective but to a lower degree than DAMP.

关 键 词：2 4-diamino-6-mercaptopyrimidine （DAMP） 2-mercaptopyrimidine （2-MP） [3-hematin Hemozoin Ferriprotopor-phyrin IX （FP） biomineralisation chloroquine diphosphate （CQ）. 

分 类 号：S831.5[农业科学—畜牧学] TQ464.9[农业科学—畜牧兽医]