The ethyl acetate-soluble portion, some of the isolated compounds and hemisynthetic derivatives were evaluated for their antiplasmodial activity against the multidrug-resistant Dd2 strain of Plasmodium falciparum
A series of novel keto-enamine chalcone-chloroquine based hybrids were synthesized following new methodology developed in our laboratory.
In the absence of secular climatic changes, the global challenges of changing epidemiological patterns of malaria have to be induced by man, i.e. by a disturbance of the equilibrium between man, vector and the parasite in an environment conducive to the natural transmission of the pathogen.
A variety of 2-(aminomethyl)aziridines was prepared and converted into the corresponding 1,2,3-triaminopropanes through a novel, microwave-assisted and regioselective ring opening by diethylamine in acetonitrile.
Dialkylaminoalkyl derivatives of 2-azabicyclo[3.2.2]nonanes and of bicyclo[2.2.2]octanes were prepared and their activities determined in vitro against the multiresistant K1 strain of Plasmodium falciparum.
This paper describes the synthesis of novel peptidomimetics bearing a protected aspartyl aldeyde warhead leading to the thioacylals 2a,b and the acylals 3a,b.
Benzo[c]phenanthridine alkaloids represent interesting lead for the discovery of new potential antiplasmodial and/or anticancer drugs. In this field, a novel library of aza-analogs of benzo[c]phenanthroline framework derivatives was designed and prepared.
ELEAB inhibited parasitaemia and enhanced mean survival time in a dose- dependent manner upto 750 mg/kg/day dose in treated mice. Further studies need to be done to isolate and characterize active constituents of extract and to study their mechanism of action.
In continuation of our efforts to find new antimalarial drugs, a systematic in vitro evaluation using a chloroquine resistant strain of Plasmodium falciparum (FcB1) was undertaken on extracts prepared from various parts of Vietnamese plants.
The results thus support, at a molecular level, the clinical use of this plant in the Bhutanese traditional medicine and identified cheilanthifoline as a potential new antimalarial drug lead.