Improvement in Aqueous Solubility in Small Molecule Drug Discovery Programs by Disruption of Molecular Planarity and Symmetry – Journal of Medicinal Chemistry (ACS Publications)

Nice review. I think this is a good approach for increasing solubility, but I do not compeltely agree with the authors’ hypothesis that the improved solubility comes mainly from crystal lattice disruption. I believe that in a lot of examples mentioned by the authors that the structural modifications result in improved interactions with water, perhaps through H-bonding. These type of effects are not seen by LogP since the non-aqueous phase (octanol) can H-bond as well.  Looking as polar surface area and/or LogPhexane would probably show this more clearly.

 

Improvement in Aqueous Solubility in Small Molecule Drug Discovery Programs by Disruption of Molecular Planarity and Symmetry – Journal of Medicinal Chemistry (ACS Publications)

via Improvement in Aqueous Solubility in Small Molecule Drug Discovery Programs by Disruption of Molecular Planarity and Symmetry – Journal of Medicinal Chemistry (ACS Publications).

Advertisements

Leave a Reply

Fill in your details below or click an icon to log in:

WordPress.com Logo

You are commenting using your WordPress.com account. Log Out / Change )

Twitter picture

You are commenting using your Twitter account. Log Out / Change )

Facebook photo

You are commenting using your Facebook account. Log Out / Change )

Google+ photo

You are commenting using your Google+ account. Log Out / Change )

Connecting to %s


%d bloggers like this: