Bluelight

Thread: I Like to Draw Pictures of Random Molecules

Page 174 of 197 FirstFirst ... 74124154164170171172173174175176177178184194 ... LastLast
Results 4,326 to 4,350 of 4911
  1. Collapse Details
     


    PSI-N-ETHYL-SHIVA



    SHIVA

    And finally, a good alternative to MDMA:



    PCA (whose effects were 'well tolerated' according to one old study)



    2C-SHIVA has already been synthed and tested. It was found to be a stimulant but not a psychotomimetic.
    Last edited by Dresden; 04-07-2017 at 19:24.
    Reply With Quote
     

  2. Collapse Details
     

    7-acetyl-mitragynine


    7-AcO-Mitragynine

    I don't know all that much about drug design nor pharmacology (yet, I really want to learn more) -- would either of these make a much more potent mitragynine analog? My logic was that being that acts on opioid receptors, something that causes opioids to be more potent (morphine -> heroin with diacetyls), it would also work for mitragynine? I chose the 7 position as a 7-HO-Mitragynine is more potent than regular mitragynine.

    Can someone explain why I'm correct/incorrect? I want to learn more about SARs and all that jazz.
    Reply With Quote
     

  3. Collapse Details
     


    beta-chloro-methamphetamine

    I realize aliphatic chloros are to be avoided, as they can N-chlorinate DNA, but some such as clindamycin are still prescribed, and let's face it, the typical user of a drug like this usually isn't the most health conscious.
    Reply With Quote
     

  4. Collapse Details
     


    Also, "indolibut"? Lmao, I don't know if this would work at all -- would it?
    Reply With Quote
     

  5. Collapse Details
     
    Sorry to double post, but has there ever been any thiophene or benzofuran analogs of LSD? If not, why?



    Reply With Quote
     

  6. Collapse Details
     
    Bluelighter Bagseed's Avatar
    Join Date
    Jul 2010
    Location
    flat spacetime
    Posts
    3,326
    might be pretty hard to synthesize.. lysergic acid after all is a compound you get from nature.
    Reply With Quote
     

  7. Collapse Details
     
    Quote Originally Posted by Dresden View Post


    beta-chloro-methamphetamine

    I realize aliphatic chloros are to be avoided, as they can N-chlorinate DNA, but some such as clindamycin are still prescribed, and let's face it, the typical user of a drug like this usually isn't the most health conscious.
    I still avoid this one, the tendency to form reactive aziridine is too strong. (leaving group at beta position to a nucleophile)
    (This is even a topic of study in Org.chem: see here for brief idea - Wiki )
    The formation is assisted by attacking of lone pair from beta-position to kick away the leaving group forming reactive three-membered ring.

    This is the principal of design of mustard gas, both sulfur and nitrogen mustard; which is much more stronger alkylating agent than a normal "chloroalkane" should have
    Reply With Quote
     

  8. Collapse Details
     


    Thought of these before giving a further look into this thread -- I saw someone propose the first one, which would be incredibly difficult to synthesize the diathiol -- or might not even be possible -- but what about the bottom two? Do you think those would be possible? An MDMA sulfur analog.
    Reply With Quote
     

  9. Collapse Details
     


    Fluoro DragonFLY
    Reply With Quote
     

  10. Collapse Details
     

    Ethoxetamine


    Acetoxetamine

    Last edited by LeviathanBaphomet; 10-07-2017 at 09:30.
    Reply With Quote
     

  11. Collapse Details
     


    PARVATI [2-amino-1-(3,4,5-trifluoropheny)-propane]
    Reply With Quote
     

  12. Collapse Details
     


    3C-DMT
    Reply With Quote
     

  13. Collapse Details
     
    Bluelighter Bagseed's Avatar
    Join Date
    Jul 2010
    Location
    flat spacetime
    Posts
    3,326
    using that nomenclature, 3C-DMT would be a,n,n-trimethyltryptamine, which is already a thing..

    is there any chance that your molecule would be active anyway?
    Reply With Quote
     

  14. Collapse Details
     


    HOT n' BLACK
    Reply With Quote
     

  15. Collapse Details
     
    Of course there's a chance 3C-DMT could be active.



    STARBUCKS
    Reply With Quote
     

  16. Collapse Details
     
    Does anyone have any insight on my mitragynine idea? I'm genuinely curious
    Reply With Quote
     

  17. Collapse Details
     
    Bluelighter Nagelfar's Avatar
    Join Date
    Nov 2007
    Location
    Vancouver, Washington USA
    Posts
    1,909
    Quote Originally Posted by aspiringdrugdesign View Post
    Does anyone have any insight on my mitragynine idea? I'm genuinely curious
    OK, let me explain why your logic here is the same as the 'methylenedioxy on everything' fallacy:
    ---
    Morphine skeleton substitution pattern and it's numbering system:

    ---


    ^Codeine, which is 3-methyl-morphine (morphine with a methyl-ether on the three position)

    way less potent than morphine & needs to me liver de-methylated (heptatic first pass metabolized) to even become morphine. It is inactive (compared to morphine activity) because the methyl's specific location blocks the mu-opioid receptor binding site with its specific/particular molecular conformation.

    ---

    Heterocodeine (6-methyl-morpine)



    ^This is a methyl on the 6 position of the morphine molecule. It doesn't block the binding site, and though it is still de-methylated by heptatic metabolism, it is six times more potent (or thereabout) than morphine because it is more structurally stable and less labile (the word "labile" can be thought of in terms of its anagram "liable" as in 'liable (to metabolize)', quicknesss with which it breaks down.
    ---
    heroin is 3,-6-acetyl (di-acetyl, or acetylated in two separate beginning places, a split in the branches each having one acetyl; as different from bi-acetyled, acetylated twice along the same branch in some sequence), now it is 1 and a half times the potency of morphine because of logP from the acetyl, it is a prodrug, most prodrugs are *less* potent because it has to become the drug, the heroin branches immediately cleave to morphine (for the most part), omitting the 3 position, and getting 6-MAM, is even more potent still, but it is more work for not so much benefit to selectively acetylate just the six position when a good yield will also react with the three position that goes bye-bye anyway upon crossing the BBB.

    Now the kratom active metabolites, how they fit the G-coupled protein receptor at mu, is different than the phenathrene morphanins.

    This answer help?
    Last edited by Nagelfar; 18-07-2017 at 20:54.
    Reply With Quote
     

  18. Collapse Details
     
    That was actually a really good read! So are SARs not really dependent on the receptor being binded to, only the structure class being modified? I really want to learn more about them or how to even understand changes in structure and their effects, but I'm unsure where to start.
    Reply With Quote
     

  19. Collapse Details
     
    Bluelight Crew Solipsis's Avatar
    Join Date
    Mar 2007
    Location
    NL
    Posts
    15,270
    Both: SAR is what makes a difference for a drug's binding to a receptor, sometimes this is generalized when a 'structure class' binds so comparably that SAR follows analogous tendencies. But you should try to not isolate one factor too much to focus on and hope or assume that the rest will stay the same. Things like lipophilicity and metabolic stability will always still be a factor and may surprise you by throwing your assumptions about a SAR pattern out of whack.
    SAR is about biological activity which is not limited to pharmacodynamics [at the receptor].

    Whether it is a good idea or not to take a structural modification like methylenedioxifying out of context really depends IMO: in doing so you may (intentionally or not) be taking a standard approach like creating an ester and it might actually not be such a bad idea..

    The methylenedioxy has mythical status for the empathogen / stimulant PEA world but it otherwise not such a common structure so often it will be silly to attach it onto some very different drug somewhere.

    Acetylating hydroxies on mitragynine may not really be useful for the lipophilicity reasons you'd acetylate opiates (actually not sure), but it might allow you to protect a group that is known to make the compounds unstable and the reason kratom extracts apparently don't have a long shelf-life (in the case of esterifying 7-hydroxy). So making the black tar heroin version of kratom alkaloids could actually be interesting? Even if inadvertently. However having to inject that seems like a terrible prospect so you would have to extract and purify to make a powder to make it snortable cause otherwise by taking it orally the acetoxy will be metabolized too much and your only benefit then may be the shelflife.

    The logic that mitragynine is an opioid may be more irrelevant than dodgy/bad when the acetylation is aimed at things like shelf-life of isolates or the log P (and thus things like absorption, pharmacokinetics etc). IMO it is not comparable to 'put a methylenedioxy on everything' because that is aimed at the SAR more often focused on: the pharmacodynamics i.e. what happens at the receptor.

    Esterifying is still not exactly universally applicable, but it is also not as case-dependent as whether a methylenedioxy has any business being on a molecule.

    On an unrelated note, and nagelfar might love this:



    Meteloidine, an alkaloid found not only in Datura/Brugmansia but I think also in Australian Erythroxylum species. AFAIK it is not known what alkaloids like these do.



    This is 1-hydroxytropacocaine I thought is found in E. Novogranatense (which I am growing a couple seedlings of), though wiki claims it is found in E. Coca.
    Last edited by Solipsis; 19-07-2017 at 13:06.
    Reply With Quote
     

  20. Collapse Details
     
    In the cumene process for acetone production it says propene.

    is it propylene gycol or propane/butanone?
    Reply With Quote
     

  21. Collapse Details
     
    It is really propene (propylene gas, for common name) ala H2C=CH-CH3

    It is the second smallest alkene, after ethene (or so called ethylene) and is a gas at room temperature and pressure.

    Didferent chemical from propylene glycol and propane or butanone...

    Wiki "propene" and look for brief
    Reply With Quote
     

  22. Collapse Details
     
    Quote Originally Posted by Pomzazed View Post
    It is really propene (propylene gas, for common name) ala H2C=CH-CH3

    It is the second smallest alkene, after ethene (or so called ethylene) and is a gas at room temperature and pressure.

    Didferent chemical from propylene glycol and propane or butanone...

    Wiki "propene" and look for brief
    See I read the articles all of them and they seemed to switch what they were talking about,but what is propylene gas?
    Reply With Quote
     

  23. Collapse Details
     
    Yes, but you will need different condition. I assume this is not synthesis discussion because conditions to control for cumene process are for industrial plants and not easily achievable in unprepared lab.

    The difference is that for propene, you use acid to protonate it making it the C3 carbocation
    In case of isopropyl alcohol, acid also protonates the hydroxyl group, the dehydration to C3 carbocation.

    After then the C3 carbocation reacts with benzene forming cumene, later steps are all the same.

    What to control is the condition (say, temp and pressure), the toxicity of benzene, the {##^*%%}smell of cumene,
    The explosive cumene hydroperoxide, the corrosive and toxic of phenol etc.

    I work in a professional org. synth wet lab, and never have an idea to "run" this process in my lab scale!
    Reply With Quote
     

  24. Collapse Details
     
    Bluelighter Bagseed's Avatar
    Join Date
    Jul 2010
    Location
    flat spacetime
    Posts
    3,326
    why would you synth acetone anyway? it is easily available.
    Reply With Quote
     

  25. Collapse Details
     
    Bluelighter Nagelfar's Avatar
    Join Date
    Nov 2007
    Location
    Vancouver, Washington USA
    Posts
    1,909
    Quote Originally Posted by Solipsis View Post

    On an unrelated note, and nagelfar might love this:
    Absolutely, thank you, as you know I'm always looking for metabolites, bio-synth precursors and relatives, and synth analogues of the like compounds
    Reply With Quote
     

Page 174 of 197 FirstFirst ... 74124154164170171172173174175176177178184194 ... LastLast

Posting Permissions

  • You may not post new threads
  • You may not post replies
  • You may not post attachments
  • You may not edit your posts
  •