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I Like to Draw Pictures of Random Molecules

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navarone:

I can't tell you much about SAR, but:

That's more of what I'd call a distant ethcathinone analogue - flourine is more like hydrogen than methyl.

Also, you can be pretty damn sure it won't metabolise like that without some funny business going on.
 
ktp said:
maybe instead of this N, put an O inside the ring: (with the only argument that many substitutions on 3 and 4 start with O anyway)

awp8nt.png


the ring is not completely flat, but looks closer to benzene than MPA's tiophene-ring:

hrgabl.png
Click to expand...

I have wondered about the pyrone analogues of amphetamine myself (as they are planar). I know a couple of routes that would probably work, but they're not terribly cheap and of course I can not discuss them here. Pyrones are fairly stable, certainly enough so to last long enough in the body to be active. I should double check scifinder and see which of these have been made.
 
nuke said:
I have wondered about the pyrone analogues of amphetamine myself (as they are planar).
Click to expand...

Is the term "planar" in chemistry here one the same with that of geometry? This thought comes to mind as ktp says its not completely "flat", and my having seen dopamine as "flat ringed" in comparison to n-methyl amphetamine. Might this answer the question I have for DA releaser + DA agonist relative to SE releaser/agonists such as ecstasy? I would assume the two hydroxys would interfere but they seem not to be included with other such DA agonists.
 
phenyldimethocaine.png


I took the phenyltropane idea to dimethocaine. It appears to be a very simplified DRI with no reason why it shouldn't work. Has this molecule ever been made? It is much like a cross between this and this. (If information is unavailable on my above posted image, does anybody have information for either chemical at either of those links?)
 
^anyone know of any drug compounds with a pyran ring?

Reckon this could be interesting:

2585jx2.png


Thieno-midazolam! Water soluble maybe?
 
^ Looks to be a little less soluble than midazolam itself (ClogP: 3.66 vs. 3.42 so it should still be water soluble), but that centre nitrogen has too many bonds! Taking a second look I realized that you just rotated those double bonds in the imidazole ring.
 
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How's this? Might this be a cannabinoid or have 5-HTergic activity?

Really random "in the margin of my anatomy and physiology class notes" type drawing.

 
The sulphur is in the opposite side of the 'ring'.
Thienodiazepinez are good enoguh as they are at the moment. they have opened a new world to GABA subunit affinity thogh they differ from one another because of their half life.
Etizolam dissapointed me a lot, brotizolam on the oher hand is an amazing drug, still it has a quite short half-life (still i think it would get hydroxylated on te diazepine ring just as diazepam does giving a still active metabilite.
 
How about this amphetamine analogue.
In £D it looks slightly non-planar compared to conventional amphetamines but considerinf the reputation of beta methoxy amphetamines (eg: phenmetrazine) and some of the reported apreciations of 2' substituted amphetamines. I thought this was a good analogue. I called it Furanamine.
59vgy9.jpg

What do you think?
 
Something else to note about S replacing O - it can be a non-reversible enzyme substrate which can be really dangerous.
 
LOL! Your bed is on the other side of the atlantic compared to mine....I'm in hte middle of the mediterrean sea. My location joke was just a spookish was to fool around.
Anyway what do you thing of my Furanamine (BTW i meant 3D by £D, lil typo)
 
Enix150 said:
^ Looks to be a little less soluble than midazolam itself (ClogP: 3.66 vs. 3.42 so it should still be water soluble), but that centre nitrogen has too many bonds! Taking a second look I realized that you just rotated those double bonds in the imidazole ring.
Click to expand...

Midazolam is unique in that the imidazole ring can open in solution (creating a highly soluble temporary form) but closes at physiological pH (7.4). Thus also demonstrating high lipid solubility (fast onset past BBB). Don't think this effect would be represented in the ClogP value. An effect very unique to midazolam.

Good point centre Nitrogen is incorrect - double bond is part of imidazole ring. :)
 
/navarone/ said:
How about this amphetamine analogue.
In £D it looks slightly non-planar compared to conventional amphetamines but considerinf the reputation of beta methoxy amphetamines (eg: phenmetrazine) and some of the reported apreciations of 2' substituted amphetamines. I thought this was a good analogue. I called it Furanamine.
59vgy9.jpg

What do you think?
Click to expand...

That's really interesting looking!
 
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