Mandeep K.

asked • 12/18/19

I need to understand the structure activity relationship of an antibiotic compound and its bioactivity

Molecule: Wollamide

Made analogs

Changed sterechem

Disk Diffusion assay

B. Subitulis

The question what is the mechanism of action of Wollamide and why other analogs didnt not work or not inhibted.


1 Expert Answer

By:

Stanton D. answered • 12/19/19

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Mandeep K.

Thank you for answering my question. Hello, I need help with a mix of microbiology/biochem/chem/bio. I did an experiment where I made mimics of TB antibiotics in a lab. I need to understand the structural activity relationship of the compound. I tested this on a bacteria as a kirby bauer disk test. The variations I made didnt inhibit the bacteria. I need to know why not and whats the mechanism of action of my compound/drug molecule. Would you be able to help? I have an idea just need verification.
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12/20/19

Stanton D.

My expertise doesn't extend to all materials active (or not!) against all kinds of various bacteria. Are you targeting M. tuberculosis, or variously distant other bacteria?
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12/21/19

Mandeep K.

I do understand, due to modifications there will be an effect on bacterial activity. I have an idea regarding the MOA, since wollamide is a cationic antimycobacterial cyclohexapeptide that exhibits activity against Mycobacterium bovis. If it’s a cyclic peptide which inhibits protein synthesis 50s of ribosome. Is it safe to assume wollamide can diffuse through the cell membrane and inhibit protein synthesis?
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12/23/19

Stanton D.

Well, diffuse through (cationic molecules easier through human cell membranes and by iontophoretic delivery through skin sweat ducts, for same reason: membranes of entry barrier have negatively-charged moieties, which provide "energy wells" for cationics to skim through, but "energy hills" to repel anionics), or maybe an active transport. But you would be interested in the M. bovis "membrane"(s), not human ones. (unless the M. bovis is encapsulated by human cells). But that all doesn't speak to the mechanism of inhibition of protein synthesis, does it?
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12/23/19

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