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Drug designs. (MedicinalUser SAR thread)

Smyth2 said:
Have you seen Besipirdine & Binedaline.
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The latter is a good example of how badly depression in human beings is so difficult to model in animal studies. There are a huge number of patents covering putative antidepressants but so often they proved to only work for a small minority of people.

I say small minority because if memory serves, even those that do receive a GSL work for less than half the people they are prescribed to. I found that a surprisingly low figure but doctors have got better at making it clear that if a given antidepressant hadn't worked after 28 days, it's appropriate to prescribe an alternative.

If memory serves amitryptaline is still the benchmark used to evaluate more modern medicines. Exactly how it works still isn't fully understood.
 
Smyth2 said:
This one reminded me of clomacran.
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But consider that ketone moiety. Unlike clomacran, those two aromatic rings are going to be planer. That's going to alter the confirmation and thus binding a lot.

As it is, the two appear to have been studied for different reasons.
 
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