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  • N&PD Moderators: Skorpio | someguyontheinternet

Drug designs. (MedicinalUser SAR thread)

Skorpio said:
I’d worry about the meta sidechain. If you had the bit that you left on your antipsychotic prototype 2 drug where the central side chain was on the first prototype, it would be promising.
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Could you design it ? I would love to see an example.
 
This is sort of what I was thinking. I added a carbon in front of the piperidine ring to get its nitrogen in a similar location to known phenothiazines, and chopped off a carbon from the propiophenone because I felt it was too long.

 
Also here is one random one I thought of: GHB triglyceride. It should cleave to GHB by the action of triacylglycerol lipases in your body being a kind of sustained release thing. No idea if it would actually work. Because it’s esterified, it wouldn’t have to be a salt.

 
The two side-chains on the same molecule reminds me of a Biriperone article though.

Chakrabarty, Ruchika; Rao, Jyoti; Anand, Aparna; Roy, Abhijeet Deb; Roy, Raja; Shankar, G.; Dua, P.R.; Saxena, Anil K. (2007). "Rational design, synthesis and evaluation of (6aR∗,11bS∗)-1-(4-fluorophenyl)-4-{7-[4-(4-fluorophenyl)-4-oxobutyl] 1,2,3,4,6,6a,7,11b,12,12a(RS)-decahydropyrazino[2′,1′:6,1]pyrido[3,4-b]indol-2-yl}-butan-1-one as a potential neuroleptic agent". Bioorganic & Medicinal Chemistry. 15 (23): 7361–7367. doi:10.1016/j.bmc.2007.07.018.
 
Skorpio said:
Also here is one random one I thought of: GHB triglyceride. It should cleave to GHB by the action of triacylglycerol lipases in your body being a kind of sustained release thing. No idea if it would actually work. Because it’s esterified, it wouldn’t have to be a salt.

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Aceburic acid would have a lowered sodium content relative to GHB.
 
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