opensourceantibiotics / Series-2-Diarylimidazoles

Open Source Antibiotics Series 2
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New compounds from NU #78

Closed lferrins closed 3 years ago

lferrins commented 3 years ago

Hi all, Quillon has been making compounds in support of our ongoing efforts and we have some surplus material that we could send your way if you are interested? The structures are below. My 2 cents on this is that, while we have declared the methoxy "death" we only have n=1 (or 2?) and I'm wondering if some of these will test that hypothesis out a bit more? Otherwise, I feel this is a good set!

S02
MFernflower commented 3 years ago

This is a nice set of compounds - We did indeed find that adding an EDG to the bicylic ring was a bad idea (so the methylsulfur compound should be inactive as a stone at-least in theory) - however it seems adding one to the pyridine system is fine see issue #76

If this batch of compounds does get made it would finalized the "dont put things on the bicyclic ring" part of the SAR so in that way i think it's useful @mattodd

@lferrins

lferrins commented 3 years ago

Thanks @MFernflower - just to clarify though, these compounds have already been made and are available to ship. We are just trying to make sure that they all make sense to ship!

MFernflower commented 3 years ago

@mattodd @danaklug Maybe we can use these to finalize this "dont put things on the bicyclic ring" rule

Need to discuss at tommrow's meeting #79

MFernflower commented 3 years ago

@lferrins How did the methoxy even wind up on the core anyway?

lferrins commented 3 years ago

@MFernflower we use a substituted aminopyridine which gives us the methoxy in the core. We have been looking at it for anti-Leish activity in our research efforts.

danaklug commented 3 years ago

These compounds have now been shipped and assigned OSA numbers (see below) and will be included in the next round of MRSA screening.

image

danaklug commented 3 years ago

Compounds have arrived at UCL, thanks @loriferrins @QSimpson !

danaklug commented 3 years ago

Closing, these structures have been folded into #84.