Pharmacology Nitazenes - The odd N-substitution of...

[4DQSAR]

I'm just wondering aloud if anyone ever tried the (S,S) 2,4-dimethyl azetidine homologue of etonitazene. I mention this because when the diethyl moirty of LSD was replaced by this chiral derivative, the result was more potent than the patent. I've also noted monosubstituted example and so it's possible that like (the S) sec-butyl homologue of LSD, it IS purely space filling as the basic nature of a secondary amine is significantly different to the basic nature of a tertiary amine.

I mean, the former is not going to be economic (so mentioning it isn't going to cause harm) but the latter might suggest that other (chiral) monosubstitutions would be even more potent although, of course, you need that chiral amine so again, it's an extra cost...

 

[izo]

Not really an answer to your question but when it comes to the N Substitution of the nitazenes i Found that the compounds with the N incorporated into a ring work quite better than These with dialkyl Substitution.

 

[4DQSAR]

Not really an answer to your question but when it comes to the N Substitution of the nitazenes i Found that the compounds with the N incorporated into a ring work quite better than These with dialkyl Substitution.

There have been a host of different N-substituuents. I'm purely interested to know if chirality is important. After all, viminol has 6 isomers but only one is an active opioid. I did the paperwork and the isomer claimed to be an antagonist wasn't - it just causes jumping in mice (which is still used to denote opioid abstainance syndrome). But I can't be bothered to alter the Wikipedia page - if you belive a source that ANYONE can alter - good luck!