Browsing by Author "Guantai, Eric"

Now showing 1 - 2 of 2
  • Thumbnail Image
    Item
    Open Access
    Curcumin-related hybrid compounds as potential antimalarial agents : design, synthesis, mechanistic investigations, biological evaluation and pharmacokinetic studies
    (2010) Guantai, Eric; Chibale, Kelly; Smith, Peter
    Malaria remains one of the most devastating tropical diseases, with staggering infection and mortality statistics. Over 200 million clinical cases of malaria (resulting in 1 - 3 million deaths) are reported annually. Africa bears the greatest burden of this disease. with the vast majority of malaria cases (>85%). and malaria-related deaths (>90%). being reported in sub-Saharan Africa. The main challenge to malaria control has been the development of clinically significant resistance Of the parasite to most known antimalarial drugs. This suggests that the development of new, highly efficadous drugs and/or treatment regimens for the management of malaria remains a key priority. This study applied molecular hybridization as a strategy in the development of novel potential antimalarial agents. The aim was to try and identify novel hybrid compounds containing scaffolds that are structurally related to the natural product curcumin, and which exhibit in vitro and in vivo antimalarial activity. Part of the study involved investigations into the pharmacokinetics and possible antimalarial mechanisms of action of selected target compounds.
  • Thumbnail Image
    Item
    Open Access
    How can natural products serve as a viable source of lead compounds for the development of new/novel anti-malarials?
    (BioMed Central Ltd, 2011) Guantai, Eric; Chibale, Kelly
    Malaria continues to be an enormous global health challenge, with millions of new infections and deaths reported annually. This is partly due to the development of resistance by the malaria parasite to the majority of established anti-malarial drugs, a situation that continues to hamper attempts at controlling the disease. This has spurred intensive drug discovery endeavours geared towards identifying novel, highly active anti-malarial drugs, and the identification of quality leads from natural sources would greatly augment these efforts. The current reality is that other than compounds that have their foundation in historic natural products, there are no other compounds in drug discovery as part of lead optimization projects and preclinical development or further that have originated from a natural product start-point in recent years. This paper briefly presents both classical as well as some more modern, but underutilized, approaches that have been applied outside the field of malaria, and which could be considered in enhancing the potential of natural products to provide or inspire the development of anti-malarial lead compounds.