BioOrganoMetallic drug chemistry

[Nagelfar]

I've been ever interested in throwing a metal(oid) on a substitution and having affinity jump due to electromagnetic considerations. I know of only two phenyltropanes, but what of a substrate? What of a benzo that has it on a space with one?

I'll add to this with the two I know when I can make it to the library.

I'm sure there's more than one example where the main binding atom, say nitrogen or oxygen, can be replaced since the steric considerations are unchanged in form, a metal there or elsewhere holds it to the ligand site without it.

 

[polymath]

In this article the authots describe some dopamine receptor direct agonists that are organometallic.

https://www.zora.uzh.ch/id/eprint/69307/1/COCHBI-D-11-00077_R1_Submission.pdf

 

[Nagelfar]

Thank you polymath (a name like that makes me think if I weren't Nagelfar even in real life with some, I might be Factotum here ;-) that or Plenipotentiary ;-P )

I want to see info on a substrate of DAT (namely n-methamp) that is pi stacked like the PTs I am thinking of, if it'd still act as a substrate and if not, whether it makes a great uptake inhibitor

 

[sekio]

most organometals are metabolically labile & are also probably toxic via introduction of metals into places they shouldn't normally be.

 

[Nagelfar]

I am interested in nonlabile: e.g. excretes the same as it entered, sandwiched on or so well bound as to not find itself intruding in a lingering fashion after it has run its gauntlet/gamut. There has to be a good example.

 

[sekio]

ferrochloroquine maybe? not CNS active but a drug with antiplasmodium acitivity

 

[Nagelfar]

I suppose even knowing two that bind to DAT is a lucky find, but at least we see it used. The electrostatic interactions really interest me, it's like having a far up the periodic hetero atom going into subjective euphoria itself. I romantically would like to imagine quantum implication. That said, a psychedelic as a serotonin agonist since, as you say this field utilizes DA receptor ligands; what'd it do, how would the complex be added for affect rather than as radioligand?

That's it though; searching for radio-ligands might yield some.