From National Geographic, there has been a lot of hype on Kelly Chibale's work from University of Cape Town on the aminopyridine MMV390048. Unfortunately, this was from an announcement from an internal meeting so there is very little literature on the compound.

So I ask, does anyone have good literature on the compound?

  • $\begingroup$ A search for "Chibale [au] AND malaria" on Pubmed returns a few results. This may be related to what you are asking for: ncbi.nlm.nih.gov/pubmed/21966980 $\endgroup$ – nico Aug 31 '12 at 20:28
  • $\begingroup$ @TomD, I believe that you have identified MMV39008. Thanks to everyone for helping me with this search! $\endgroup$ – bobthejoe Sep 5 '12 at 5:55

I don't know anything about this topic, but I did find this recent paper:

Kamaljit Singh,Hardeep Kaur, Kelly Chibale, Jan Balzarini, Susan Little, Prasad V. Bharatam (2012) 2-Aminopyrimidine based 4-aminoquinoline anti-plasmodial agents. Synthesis, biological activity, structure–activity relationship and mode of action studies. European Journal of Medicinal Chemistry 52:82–97

The authors analyse a range of compounds for in vitro anti-plasmodial activity. The most active is named 5-isopropyloxycarbonyl-6-methyl-4-(2-nitrophenyl)-2-[(7-chloroquinolin-4-ylamino)butylamino] pyrimidine (referred to as 10r in the paper).

Although the code name MMV390048 does not appear in the paper the strategy that this group is following is discussed in detail. My guess would be that MMV390048 is a development of 10r.

This is the structure of 10r as depicted in Table 1 of the paper:

structure of 10r


It turns out that TomD is the winner. That particular paper is an amino-pyridine class and exhibits single-dose efficacy. Amazingly, the other two papers mentioned by Satz and Alan Boyd are leads for other classes of compounds with Satz's paper focused on an amodiaquine derivative and Alan's paper focused on an alternative 2 amino-pyridine backbone also based off amodiaquine.

3,5-Diaryl-2-aminopyridines as a Novel Class of Orally Active Antimalarials Demonstrating Single Dose Cure in Mice and Clinical Candidate Potential



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