Friday, 30 May 2014

Bio precursors and their Importance

A precursor is a compound that participates in the chemical reaction that produces another compound. In biochemistry, the term "precursor" is used more specifically to refer to a chemical compound preceding another in a metabolic pathway. The first ever bio precursor was made for Malaria.

Plasmodium falciparum is responsible of the most severe form of malaria, and new targets and novel chemotherapeutic scaffolds are needed to fight emerging multidrug-resistant strains of this parasite. Bis-alkylguanidines have been designed to mimic choline, resulting in the inhibition of plasmodial biosynthesis. 

Despite potent in vitro antiplasmodial and in vivo antimalarial activities, a major downside of these compounds for advance clinical growth is their short oral bioavailability. To explain this issue, several modulations were performed on bis-alkylguanidines. The introduction of N-disubstituents on the guanidine motif amended both in vitro and in vivo activities. On the other hand, in vivo pharmacological assessment in a mouse model showed that the N-hydroxylated derivatives constitute the first oral bioprecursors in bis-alkylguanidine sequences.

The article Design and Applications of Bioprecursors: A Retrometabolic Approach has given detailed information about bio precursor and their link for it to be a Retrometabolic approach. Also, the journal Current Drug Metabolism focuses on the roots of pharmacokinetics and pharmacodynamics.

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