When looking at a novel opioid, I've always used the levorphanol & fentanyl scaffold to overlay. Even things like Viminol Do overlay, or at least it follows the 4-sites identified-
1 x aromatic system
2 x hydrogen bond donors
1 x positively ionizable function
All of the high-potency opioids have 2 aromatics or similar (lipophilic) group. Fentanyl, PET-7 and etonitezine are all examples.
I have 1 single case where I cannot work out the overlay - it's tilidine. Tilidine is unusual in many ways overlaying cypenamine as it does, secondary amine being active and NOT going anywhere the Morphine Rule
1 - aromatic system
2 - quaternary carbon
3 - ethylene spacer
4 - tertiary amine
Well, it follows 1 of the rules, I guess. Has anyone with Chemoffice overlayed nortilidine & levorphanol? Anyone already solved this one, I would love to know. It's very unlikely to lead to a potent drug and precursors cost a fortune so to make this 100% clear, I'm really just interested in the overlay, not in anything else.
Cheers
1 x aromatic system
2 x hydrogen bond donors
1 x positively ionizable function
All of the high-potency opioids have 2 aromatics or similar (lipophilic) group. Fentanyl, PET-7 and etonitezine are all examples.
I have 1 single case where I cannot work out the overlay - it's tilidine. Tilidine is unusual in many ways overlaying cypenamine as it does, secondary amine being active and NOT going anywhere the Morphine Rule
1 - aromatic system
2 - quaternary carbon
3 - ethylene spacer
4 - tertiary amine
Well, it follows 1 of the rules, I guess. Has anyone with Chemoffice overlayed nortilidine & levorphanol? Anyone already solved this one, I would love to know. It's very unlikely to lead to a potent drug and precursors cost a fortune so to make this 100% clear, I'm really just interested in the overlay, not in anything else.
Cheers