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Pharmaceuticals

Antimalaria Drugs

July 19, 2010 | APPEARED IN VOLUME 88, ISSUE 29

Reviving the malaria fight with “open innovation” after public disclosure of potential antimalarial leads by the pharmaceutical consortium is a great idea (C&EN, May 24, page 11). I truly thank them. This open innovation should provide new impetus to revisit some specific parasite targets such as the malaria CDK (cyclin-dependent kinases).

A few years ago, my group at Walter Reed Army Institute of Research published two articles showing a 3-D pharmaco­phore model for inhibition of a Plasmodium falciparum CDK (also known as Pfmrk) developed from a set of several structurally diverse kinase inhibitors with a wide range of activity (J. Med. Chem. 2004, 47, 5418; Expert Opin. Drug Discov. 2007, 2, 1115). Using the model as a search template for virtual screening of compound databases, we were able to discover 16 new potent Pfmrk inhibitors.

The compound (SJ000025081) shown in the C&EN article maps perfectly well onto our published pharmacophore model and predicts excellent antimalarial activity. Thus the model may be a useful tool for rapid selection of inhibitors for the malarial kinases.

Apurba K. Bhattacharjee
Silver Spring, Md.

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