Chemistry-Related Hijinks, Hoopla, and Skullduggery - Since 2011
Friday, June 15, 2012
Adventures in Publication: Malaria Sandwich
Hot on the heels of the recent ferrocene-based carbonic anhydrase inhibitors (see Pipeline or Chemistry Blog for more perspective) comes a few more medicinally-inclined sandwich compounds. Published in back to backASAPs, the new leads stitch together an antimalarial quinoline and a glycoside with some ferrocenyl 'Scotch tape.' The resulting "novel trifunctional conjugates" purport to treat chloroquine-resistant P. falciparum strains with low-micromolar potency.
Chirality? At that carbon?
A few salient questions: First, if these compounds represent med-chem advances, why are they in Organometallics, of all places? Surely this wasn't the first Editor's desk they landed upon! Second, both papers seem to be variations on a theme, so why not just combine them and make one stronger paper? Lastly, can anyone interpret the stereochemistry shown in this intermediate? It's drawn to suggest a chiral acetal; my o-chem 'spider sense' says that cannot be.
To my med-chem inclined readers: what do you make of these molecules? Bandwagon hype, or real advance?
Update, 6/15/12 - Changed figure caption, and "ketal" to "acetal"