Isolation and modification of pseudohybrid plant (Lupeol)
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ABSTRACT:
To start with, a brief introduction has been presented on Malaria as a serious endemic disease and the need to develop new structural classes of antimalarial agents with novel and different mechanism of action. Stress has been given to the fast emerging multidrug resistance of P.falciparum to the commonly used drug chloroquine. Crateva nurvala (Capparidaceae) is a plant from which Lupeol has been isolated and its reported antimalarial activity prompted to prepare semisynthetic derivatives for development of new antimalarial agent for better activity. In the treatment of malaria, natural produts are unending source of new lead and their role is not new. The structure of Lupeol is reminiscent of that of cholesterol, and the compound is expected to be able to enter the cellular membranes. Due to the presence of a single hydroxy group and a large, apolar skeleton, and Lupeol acts as an amphiphile. According to the bilayer hypothesis Stomatocytes are generally formed when a lipophilic compound is incorporated into and expands the inner layer of the lipid membrane .Such changes appear to be
more prohibiting with respect to parasite growth than incorporation of an amphiphile into the outer layer, as in
case of echinocytogenic compounds. The two possible sites for chemical modification present in Lupeol are ring-A, and isopropenyl side chain. Modification on ring-A, ring-A expansion and cleavage followed by introduction of antimalarial pharmacophores and modification at isopropenyl side chain is targeted as represented in 1 a.
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