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Topic: Nitrofuran reactivity  (Read 8951 times)

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Offline Borek

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Re: Nitrofuran reactivity
« Reply #15 on: May 23, 2010, 09:13:06 AM »
Borek I don’t see how is sarcasm constructive approach especially when it is completely wrong.

It is not wrong. You are assuming that nitro group can be modified in many ways and that we are limited only by imagination. I gave you several examples of things where our imagination completely doesn't matter - matter has its own ways. Same here - we know how nitro group can be modified, as generations of chemists tried to modify them in a fancy way. If they have not succeded that's not because of lack of efforts, that's because imagination is not enough, you need cooperating matter.
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Offline orgopete

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Re: Nitrofuran reactivity
« Reply #16 on: May 24, 2010, 10:18:29 AM »
Major modifications are readily possible, but I presume that would result in an inactive drug. I am presuming that would not be of interest. Is that correct?

I’m actually looking for inactive drug. What we are aiming for is inactivation by modification of nitro group of nitrofuran part of molecules.
Those modifications are actually what I'm looking for.

Since you have access to many bacterial strains, what is the problem with using one of the active ingredients?

The problem is that those drugs are active and resistant strains that we have are mutants in ways that are not useful for this study. This is a problem for finding such variation. I was looking into patent application and analogs, but thing is that there it is not so likely finding some patent for inactive compounds. Simply people don’t want to pay for thing without possibility to earn some money back.
The reason I did not expect this answer was I presumed the enzyme paradigm suggested by Pauling is correct. That is, enzymes work by reducing the activation energy of a reaction and that mimics of this intermediate can serve as inhibitors of the reaction. As we become increasingly sophisticated about the structures for given targets, unexpectedly small changes can result in compounds that are not inhibitors, that is they do not bind to the active site.

This reminds me of the movie, Five Easy Pieces, in which Jack Nicholson orders toast by ordering a bacon, lettuce, and tomato sandwich and leaves out the bacon, lettuce, and tomato. Leave out the compound or substitute it with nitrobenzene, toluene, anything, and it will be inactive. I just don't understand how this would be helpful to you.

I will guess that it would be a surprise to you that if you had all of the compounds claimed or described in a patent and tested them that they would not contain the same level of biological activity and that some of the compounds may in fact be nearly or completely inactive. However, companies are reluctant to disclose the structure activity relationship of those compounds. That would aid competitors to get that information without any work on their part. (If you are paying attention though, you actually can perform a quasi-qsar analysis and you may be able to detect inactive or weakly active isomers in the patent.)

I still do not understand the scientific principle that is guiding this research.
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Offline OC pro

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Re: Nitrofuran reactivity
« Reply #17 on: May 24, 2010, 04:37:01 PM »
"I still do not understand the scientific principle that is guiding this research. "

There is none. Money is the driving force.

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