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

作者:Vlasceanu Alexandru; Jessing Mikkel; Kilburn John Paul*
来源:Bioorganic & Medicinal Chemistry, 2015, 23(15): 4453-4461.
DOI:10.1016/j.bmc.2015.06.019

摘要

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.

  • 出版日期2015-8-1