4 thoughts on “D16 – O’Neal

    1. This is such a good question! And honestly it’s probably beyond my scope (would be fascinated to hear a medicinal chemist talk about this). Our primary method of modification in this context was dilution, but since this medication currently exists as an eye drop, and since most ingested antibiotics need to ultimately be bioavailable in serum, I suspect using medicinal chemistry to alter solubility would be a good place to start!

  1. Since neither the max or 5 dilutions demonstrated anti-biotic activity, which ways would yopu combine it with other drugs to make it easier to administer or effective?

    1. Thanks for this question! Since we know the method of action for this medication is as a carbonic anhydrase inhibitor, and since we know that beta carbonic anhydrase is important in bacterial function, I suspect that the poor efficacy we see might be because it’s not able to reliably enter the bacterial cytosol. Some antibiotics (like ampicillin, our positive control, and like most beta-lactam antibiotics) work really well by penetrating bacteria cell walls. I think it would be interesting to pair those two, to see if brinzolamide could potentiate that activity and make an existing antibiotic either more effective, or more difficult to develop resistance to.

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