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Antimalarial and antimicrobial activities of 8-Aminoquinoline-Uracils metal complexes.

Phopin K, Sinthupoom N, Treeratanapiboon L, Kunwittaya S, Prachayasittikul S, Ruchirawat S, Prachayasittikul V - EXCLI J (2016)

Bottom Line: 8-Aminoquinoline (8AQ) derivatives have been reported to have antimalarial, anticancer, and antioxidant activities.Interestingly, all of these metal complexes (1-6) showed fair antimalarial activities.The results reveal application of 8AQ and its metal complexes as potential compounds to be further developed as novel antimalarial and antibacterial agents.

View Article: PubMed Central - PubMed

Affiliation: Center for Research and Innovation, Faculty of Medical Technology, Mahidol University, Bangkok 10700, Thailand; Department of Clinical Microbiology and Applied Technology, Faculty of Medical Technology, Mahidol University, Bangkok 10700, Thailand.

ABSTRACT
8-Aminoquinoline (8AQ) derivatives have been reported to have antimalarial, anticancer, and antioxidant activities. This study investigated the potency of 8AQ-5-substituted (iodo and nitro) uracils metal (Mn, Cu, Ni) complexes (1-6) as antimalarial and antimicrobial agents. Interestingly, all of these metal complexes (1-6) showed fair antimalarial activities. Moreover, Cu complexes 2 (8AQ-Cu-5Iu) and 5 (8AQ-Cu-5Nu) exerted antimicrobial activities against Gram-negative bacteria including P. shigelloides and S. dysenteriae. The results reveal application of 8AQ and its metal complexes as potential compounds to be further developed as novel antimalarial and antibacterial agents.

No MeSH data available.


Chemical structures of primaquine, tafenoquine, sitamaquine and NPC1161
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Figure 1: Chemical structures of primaquine, tafenoquine, sitamaquine and NPC1161

Mentions: Primaquine, 8-aminoquinoline (8AQ) analog, is approved by the Food and Drug Administration (FDA) for the treatment of relapses in Plasmodium infections (Hill et al., 2006[10]). It exhibits antimalarial activity against P. vivax, P. ovale and P. falciparum (White et al., 2014[41]). In addition, tafenoquine is the 8AQ drug being developed for P. vivax that is currently in clinical trials (Nasveld et al., 2010[23]). However, the usage of these 8-aminoquinolines is limited because they are likely to cause red blood cell hemolysis in patients with glucose-6-phosphate dehydrogenase (G6PD) deficiency (Bolchoz et al., 2001[3]). Regarding safety treatment and prevention of hemolytic anemia, patients with malarial infection should be screened for G6PD deficiency before treating with these medicines. Moreover, 8-aminoquinolines (sitamaquine and NPC1161) have been shown to be active against Leishmania and Trypanosoma parasites (Kulshrestha et al., 2011[17]; Yardley et al., 2010[42]). Thus, searching for novel potential bioactive compounds is required for the treatment of malaria-infected patients. These drugs/compounds (Figure 1(Fig. 1)) are 8-AQ derivatives in which their 8-NH2 groups are substituted with various alkylamines side chain (Yardley et al., 2010[42]; Jain et al., 2005[11]; Kaur et al., 2007[15]) including bis (8-AQs) (Kaur et al., 2011[14]).


Antimalarial and antimicrobial activities of 8-Aminoquinoline-Uracils metal complexes.

Phopin K, Sinthupoom N, Treeratanapiboon L, Kunwittaya S, Prachayasittikul S, Ruchirawat S, Prachayasittikul V - EXCLI J (2016)

Chemical structures of primaquine, tafenoquine, sitamaquine and NPC1161
© Copyright Policy - open-access
Related In: Results  -  Collection

License
Show All Figures
getmorefigures.php?uid=PMC4834669&req=5

Figure 1: Chemical structures of primaquine, tafenoquine, sitamaquine and NPC1161
Mentions: Primaquine, 8-aminoquinoline (8AQ) analog, is approved by the Food and Drug Administration (FDA) for the treatment of relapses in Plasmodium infections (Hill et al., 2006[10]). It exhibits antimalarial activity against P. vivax, P. ovale and P. falciparum (White et al., 2014[41]). In addition, tafenoquine is the 8AQ drug being developed for P. vivax that is currently in clinical trials (Nasveld et al., 2010[23]). However, the usage of these 8-aminoquinolines is limited because they are likely to cause red blood cell hemolysis in patients with glucose-6-phosphate dehydrogenase (G6PD) deficiency (Bolchoz et al., 2001[3]). Regarding safety treatment and prevention of hemolytic anemia, patients with malarial infection should be screened for G6PD deficiency before treating with these medicines. Moreover, 8-aminoquinolines (sitamaquine and NPC1161) have been shown to be active against Leishmania and Trypanosoma parasites (Kulshrestha et al., 2011[17]; Yardley et al., 2010[42]). Thus, searching for novel potential bioactive compounds is required for the treatment of malaria-infected patients. These drugs/compounds (Figure 1(Fig. 1)) are 8-AQ derivatives in which their 8-NH2 groups are substituted with various alkylamines side chain (Yardley et al., 2010[42]; Jain et al., 2005[11]; Kaur et al., 2007[15]) including bis (8-AQs) (Kaur et al., 2011[14]).

Bottom Line: 8-Aminoquinoline (8AQ) derivatives have been reported to have antimalarial, anticancer, and antioxidant activities.Interestingly, all of these metal complexes (1-6) showed fair antimalarial activities.The results reveal application of 8AQ and its metal complexes as potential compounds to be further developed as novel antimalarial and antibacterial agents.

View Article: PubMed Central - PubMed

Affiliation: Center for Research and Innovation, Faculty of Medical Technology, Mahidol University, Bangkok 10700, Thailand; Department of Clinical Microbiology and Applied Technology, Faculty of Medical Technology, Mahidol University, Bangkok 10700, Thailand.

ABSTRACT
8-Aminoquinoline (8AQ) derivatives have been reported to have antimalarial, anticancer, and antioxidant activities. This study investigated the potency of 8AQ-5-substituted (iodo and nitro) uracils metal (Mn, Cu, Ni) complexes (1-6) as antimalarial and antimicrobial agents. Interestingly, all of these metal complexes (1-6) showed fair antimalarial activities. Moreover, Cu complexes 2 (8AQ-Cu-5Iu) and 5 (8AQ-Cu-5Nu) exerted antimicrobial activities against Gram-negative bacteria including P. shigelloides and S. dysenteriae. The results reveal application of 8AQ and its metal complexes as potential compounds to be further developed as novel antimalarial and antibacterial agents.

No MeSH data available.