mad_scientist
Bluelighter
- Joined
- Apr 20, 2006
- Messages
- 619
Now i know theres not really much need to design new benzos seeing as there are so many different ones already, but they are a class of drug which are quite popular and drug design is always a good topic...
From some website i found...
Now i thought its good to look at which benzos are most abused as this will allow us to decide what substitution patterns are best. Benzos that have specific treatment by the law in various countries, or have a reputation among doctors as being particularly subject to abuse, include Temazepam, Triazolam, Nimetazepam, Flunitrazepam and Bromazepam. Other ones which people seem to enjoy judging by what people say on here are Midazolam, Alprazolam, Nitrazepam, Clonazepam, Phenazepam and Brotizolam.
For the substituent at the 7-position, a nitro or bromo seems to be best, probably nitro as all four benzos with a nitro group at this position are known for being particularly subject to abuse. I am curious about a trifluoromethyl group at this position though as it doesn't appear to have been tried, and trifluoromethyl often makes a good alternative to chloro.
On the 2' position of the second phenyl ring, halogens boost the activity, but also seem to boost amnesia, chloro a little bit but fluoro at this position makes for a highly amnesiac drug in every case. However im also intrigued by bromazepam which has a heterocyclic nitrogen at this position (phenyl ring replaced by 2-pyridine) as the data sheet says this increases water solubility and shortens activity, both of which are good characteristics for a recreational drug.
On the nitrogen at the 1-position, methylated drugs definitely seem to be preferred to non-methylated where both choices have been marketed (i.e. nimetazepam vs nitrazepam, temazepam vs oxazepam). However the triazolo substitution on this position also seems to be quite popular, boosts activity considerably and shortens activity, although its debatable as to whether it makes for a more enjoyable drug or not.
So my pick is for a nitro at the 7-position, a heterocyclic nitrogen at the 2'-position, and a triazolo group around the nitrogen at position 1. Proposed compound is 1-Methyl-8-nitro-6-pyridin-2-yl-4H-2,3,5,10b-tetraaza-benzo[e]azulene, think i'll call it Pynitrazolam. Synthesis should be straightforward adaptation of published routes to other known benzos, and it should be legal throughout most of the world...
Anyone else got any ideas?
From some website i found...
Now i thought its good to look at which benzos are most abused as this will allow us to decide what substitution patterns are best. Benzos that have specific treatment by the law in various countries, or have a reputation among doctors as being particularly subject to abuse, include Temazepam, Triazolam, Nimetazepam, Flunitrazepam and Bromazepam. Other ones which people seem to enjoy judging by what people say on here are Midazolam, Alprazolam, Nitrazepam, Clonazepam, Phenazepam and Brotizolam.
For the substituent at the 7-position, a nitro or bromo seems to be best, probably nitro as all four benzos with a nitro group at this position are known for being particularly subject to abuse. I am curious about a trifluoromethyl group at this position though as it doesn't appear to have been tried, and trifluoromethyl often makes a good alternative to chloro.
On the 2' position of the second phenyl ring, halogens boost the activity, but also seem to boost amnesia, chloro a little bit but fluoro at this position makes for a highly amnesiac drug in every case. However im also intrigued by bromazepam which has a heterocyclic nitrogen at this position (phenyl ring replaced by 2-pyridine) as the data sheet says this increases water solubility and shortens activity, both of which are good characteristics for a recreational drug.
On the nitrogen at the 1-position, methylated drugs definitely seem to be preferred to non-methylated where both choices have been marketed (i.e. nimetazepam vs nitrazepam, temazepam vs oxazepam). However the triazolo substitution on this position also seems to be quite popular, boosts activity considerably and shortens activity, although its debatable as to whether it makes for a more enjoyable drug or not.
So my pick is for a nitro at the 7-position, a heterocyclic nitrogen at the 2'-position, and a triazolo group around the nitrogen at position 1. Proposed compound is 1-Methyl-8-nitro-6-pyridin-2-yl-4H-2,3,5,10b-tetraaza-benzo[e]azulene, think i'll call it Pynitrazolam. Synthesis should be straightforward adaptation of published routes to other known benzos, and it should be legal throughout most of the world...
Anyone else got any ideas?
