Format

Send to

Choose Destination
Bioorg Med Chem. 2015 Aug 1;23(15):4453-61. doi: 10.1016/j.bmc.2015.06.019. Epub 2015 Jun 15.

BN/CC isosterism in borazaronaphthalenes towards phosphodiesterase 10A (PDE10A) inhibitors.

Author information

1
Department of Chemistry, University of Copenhagen, Universitetsparken 5, 2100 Copenhagen, Denmark.
2
Discovery Chemistry and DMPK, H. Lundbeck A/S, Ottiliavej 9, 2500 Valby, Denmark.
3
Discovery Chemistry and DMPK, H. Lundbeck A/S, Ottiliavej 9, 2500 Valby, Denmark. Electronic address: JPK@lundbeck.com.

Abstract

The application of BN/CC isosterism is explored as a method of expanding the scope of core scaffolds in biologically active compounds. The viability of potential drug candidates incorporating BN-heteroaromatic moieties was investigated through the synthesis of BN-substituted analogs to known phosphodiesterase (PDE10A) inhibitors, namely MP10 and a selection of N-methylanilide analogs. These in some cases revealed unexpectedly potent and relatively stable derivatives, providing further support for the potential of BN-incorporation in medicinal chemistry.

KEYWORDS:

Antipsychotics; Borazaronaphthalenes; PDE10A inhibitors

PMID:
26113188
DOI:
10.1016/j.bmc.2015.06.019
[Indexed for MEDLINE]

Supplemental Content

Full text links

Icon for Elsevier Science
Loading ...
Support Center