Boron therapeutics at Anacor

I gave a talk at Anacor Pharmaceuticals today, a company located in the Palo Alto area (which is pretty much in the Silicon Valley), not far away from San Francisco. Dr. Vincent Hernandez was my host. Anacor has been in existence for about a decade and, over the years, managed to convince both academic and drug discovery worlds of the virtues of boron-containing therapeutics. In many of Anacor’s studies, success boils down to clever use of the so-called benzoxaborole, a heterocycle equipped with an electrophilic boron centre. Then magic happens:

http://aac.asm.org/content/57/3/1394.long

Here is a representative molecule developed at Anacor and its genesis, the benzoboroxazole nucleus. The pinkish tetrahedral atom you see in the crystal structure is boron, caught in the act of inhibiting bacterial leucyl-tRNA synthetase. The formation of this adduct with the sugar diol accounts for the observed activity of these molecules against Gram-negative bacteria.Image

Image

We are keen to collaborate with Anacor and apply the novel heterocycles I blogged about towards structure – driven antibacterial discovery. Adam and Victoria (she is about to start officially in a couple of weeks, very excited about this!) have been working on some novel boron heterocycles. I think people will like them.

 

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