xionoland
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Is it fentanyl analogs or derivates?
Hello. I am wondering if fentanyl analogs like alphamethylfentanyl is analogs or derivates of fentanyl? I find this description about the differents
of analogs and derivates written by a scientist:
For Drug discovery scientists in no longer Serendipity. They are always looking for modifications of existing drugs, potential leads etc. For a
medicinal chemist, derivative means a side chain change (modification) like from a alcohol to ester.
Analogue means that there is a modification in the backbone/Core structure it self. E.g a Core with napthalene ring modified to have core with
Quinazoline. (just an example)
You can also refer to this nice book if you really want to understand all about analogues
Analogue-based Drug Discovery Wiley Publication
IUPAC (Editor), Janos Fischer (Editor), C. Robin Ganellin (Editor)
ISBN: 978-3-527-31257-3
Hardcover 606 pages March 2006
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solo
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Analogue-based Drug Discovery Wiley Publication
Janos Fischer (Editor), C. Robin Ganellin (Editor)
Uploaded with ImageShack.us
http://ifile.it/4rx5to
* Publisher: Wiley-VCH
* Number Of Pages: 606
* Publication Date: 2006-03-31
* Sales Rank: 406236
* ISBN / ASIN: 3527312579
* EAN: 9783527312573
* Binding: Hardcover
* Manufacturer: Wiley-VCH
* Studio: Wiley-VCH
* Average Rating:
* Total Reviews:
Book Description:
The first authoritative overview of past and current strategies for successful drug development by analog generation, this unique resource spans all
important drug classes and all major therapeutic fields, including histamine antagonists, ACE inhibitors, beta blockers, opioids, quinolone
antibiotics, steroids and anticancer platinum compounds.
Of the 19 analog classes presented in detail, 9 are described by the scientists who discoverd them.
The book includes a table of the most successful drug analogs as based on the IMS ranking and compares them in terms of chemical structure, mode of
action and patentability.
It's better to die on your feet, than live on your knees....Emiliano Zapata.
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fledarmus
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Quote: Originally posted by xionoland  | For a medicinal chemist, derivative means a side chain change (modification) like from a alcohol to ester.
Analogue means that there is a modification in the backbone/Core structure it self. E.g a Core with napthalene ring modified to have core with
Quinazoline. (just an example)
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Speaking as a medicinal chemistry, I don't think this definition is quite accurate. For me at least, and for the other medicinal chemists with whom I
converse, a "derivative" of fentanyl would be something that was synthesized from fentanyl - ie, from a reaction or reaction sequence that had
fentanyl as a starting material. An "analog" of fentanyl would be something that has a structure similar to fentanyl and that might be assumed to
interact in the body the same way that fentanyl does. It might and might not be synthesized from fentanyl as a starting material.
So some analogs of a compound might also be derivatives of that compound, and many derivatives of a compound would be considered analogs of that
compound.
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albqbrian
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In the US...
for legal matters on this topic we have:
The Analog Drug Act
Now it's a legal definition. It's to cover any change to a base structure (eg. 3,4,5 trimethoxyphenylethylamine to 3,4,6). That way drugs can't be
made legal by keeping them one change ahead of current legislation.
I say the above is how I always thought of analog. Derivative, on the other hand, implied it came from a common "source". Though I would guess lots of
times these two would thus overlap.
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jon
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yeah but when you look at how the analog act is enforced the law is so vauge it's done on a case by case basis.
it has to meet 2 of 3 prongs.
1 structurally similar
2 pharmacologically similar
3 intended to be used/sold as a drug.
so you get around this by deviating from the strict federal definition of an "analog"
like one methyl group off for example
you make a homolog
several carbons and oxygens tacked on = legal as sea salt
you have to proove 2 and 3
the law really is'nt being vigorously enforced right now.
there have been a few examples made to scare everyone else.
as long as you don't advertise it online and chat with some dea agent about how it gets you high, it makes the case an uphill battle.
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