Development of new and more powerful antimalarial drugs has become more complex because of emergence of multidrug resistant strains of P. falciparum. Due to resistance of malaria parasite against well-known available drugs, the chemotherapy of malaria has become more complex and challenging. In this review we have discussed the life cycle of malaria parasite followed by quinoline based antimala...

A series of protein farnesyltransferase inhibitor ester prodrugs of FTI-2148 (17) were synthesized in order to evaluate the effects of ester structure modification on antimalarial activity and for further development of a farnesyltransferase inhibitor with in vivo activity. Evaluation against P. falciparum in red blood cells showed that all the investigated esters exhibited significant antimala...

Synthesis of novel aminoquinoline derivatives has been accomplished and their activity against malaria strains examined. The compounds showed moderate in vitro antimalarial two P. falciparum strains, 3D7 (CQ susceptible clone) Dd2 resistant clone). Three aminoquinolines were further examined for efficacy a mouse model using modified Thompson test. In this model, mice infected with berghei-infec...

OBJECTIVES to investigate the anti-kinetoplastid activity of choline-derived analogues with previously reported antimalarial efficacy. METHODS from an existing choline analogue library, seven antimalarial compounds, representative of the first-, second- and third-generation analogues previously developed, were assessed for activity against Trypanosoma and Leishmania spp. Using a variety of te...

Five pregnane glycosides were isolated from Caralluma tuberculata (1-5), in addition to a known one (russelioside E, 6). The structures of the isolated compounds were elucidated by the analysis of NMR data and FAB-MS experiments. All the isolated compounds were tested for their antimalarial and antitrypanosomal activities as well as their cytotoxicity against human diploid embryonic cell line (...

Department of Pharmacology, Efforts to discover and develop new antimalarial drugs have increased dramatically in recent Maulana Azad Medical College, years mainly because of resistance to existing antimalarial drugs. Selection of candidate drugs Bahadur Shah Zafar Marg, for clinical trials in man and the design of clinical protocols are based upon consideration of Delhi110002. data from a batt...

Malaria is still the most destructive and dangerous parasitic infection in many tropical and subtropical countries. The burden of this disease is getting worse, mainly due to the increasing resistance of Plasmodium falciparum against the widely available antimalarial drugs. There is an urgent need for new, more affordable and accessible antimalarial agents possessing original modes of action. N...

Malaria remains a major world health problem following the emergence and spread of Plasmodium falciparum that is resistant to the majority of antimalarial drugs. This problem has since been aggravated by a decreased sensitivity of Plasmodium vivax to chloroquine. This review discusses strategies for evaluating the antimalarial activity of new compounds in vitro and in animal models ranging from...

Two new sulfur-containing compounds, trans-3-methylsulfonyl-2-propenol (1) and trans-3-methylsulfinyl-2-propenol (2) were isolated together with trans-3-methylthioacrylamide (3), entadamide A (4) and entadamide C (5) from the leaves of Clinacanthus siamensis. The structures were established on the basis of the spectroscopic data. The compounds were tested for antimalarial and antimycobacterial ...

Antimalarial drugs with the 4-aminoquinoline scaffold such as the important drugs, chloroquine (CQ) and amodiaquine (AQ), have been used to prevent and treat malaria for many years. The importance of these drugs is related to their simple usage, high efficacy, affordability, and cost-effectiveness of their synthesis. In recent years, with the spread of parasite resistance to CQ and cross-resist...