Ironjustic
Thu, Jun-22-06, 17:17
<<snip>> these compounds may inhibit the parasite growth by
iron chelation mechanism <<snip>>
Design, synthesis and antimalarial activity of a new class of
iron chelators. Solomon VR, Haq W, Puri SK, Srivastava K,
Katti SB Med Chem. 2006 Mar ; 2(2): 133-8
Iron is crucial for many biochemical reactions involved in the
growth and multiplication of the malaria parasite Plasmodium
falciparum. There are many reports indicating that the iron
chelators have antimalarial activity in vitro, in vivo and in
human studies. However, these compounds suffer from a number
of serious problems such as limited membrane permeability,
short half-life and require long subcutaneous infusions. To
circumvent these drawbacks we have designed a new class of
iron chelators, wherein EDTA is tethered to 4-aminoquinoline.
Here 4-aminoquinoline scaffold is used as a carrier to
penetrate biological membrane and facilitate targetting the
compounds to acidic food vacuole of the parasite. This study
describes the synthesis of novel iron chelators and their in
vitro antimalarial activity against P. falciparum strain of
NF-54. The calculated LogP values of these compounds suggest
the importance of lipophilicity for the antimalarial activity.
The EDTA esters are more active than the corresponding acids.
The biophysical studies suggest that these compounds may
inhibit the parasite growth by iron chelation mechanism.
Who loves ya. Tom
Jesus Was A Vegetarian! http://jesuswasavegetarian.7h.com
Man Is A Herbivore! http://tinyurl.com/a3cc3
DEAD PEOPLE WALKING http://tinyurl.com/zk9fk
iron chelation mechanism <<snip>>
Design, synthesis and antimalarial activity of a new class of
iron chelators. Solomon VR, Haq W, Puri SK, Srivastava K,
Katti SB Med Chem. 2006 Mar ; 2(2): 133-8
Iron is crucial for many biochemical reactions involved in the
growth and multiplication of the malaria parasite Plasmodium
falciparum. There are many reports indicating that the iron
chelators have antimalarial activity in vitro, in vivo and in
human studies. However, these compounds suffer from a number
of serious problems such as limited membrane permeability,
short half-life and require long subcutaneous infusions. To
circumvent these drawbacks we have designed a new class of
iron chelators, wherein EDTA is tethered to 4-aminoquinoline.
Here 4-aminoquinoline scaffold is used as a carrier to
penetrate biological membrane and facilitate targetting the
compounds to acidic food vacuole of the parasite. This study
describes the synthesis of novel iron chelators and their in
vitro antimalarial activity against P. falciparum strain of
NF-54. The calculated LogP values of these compounds suggest
the importance of lipophilicity for the antimalarial activity.
The EDTA esters are more active than the corresponding acids.
The biophysical studies suggest that these compounds may
inhibit the parasite growth by iron chelation mechanism.
Who loves ya. Tom
Jesus Was A Vegetarian! http://jesuswasavegetarian.7h.com
Man Is A Herbivore! http://tinyurl.com/a3cc3
DEAD PEOPLE WALKING http://tinyurl.com/zk9fk