Design, synthesis and pharmacological evaluation of novel polycyclic heteroarene ethers as PDE10A inhibitors: Part I.

@article{Das2014DesignSA,
  title={Design, synthesis and pharmacological evaluation of novel polycyclic heteroarene ethers as PDE10A inhibitors: Part I.},
  author={Sanjib Das and Rajendra L Harde and Dnyaneshwar E Shelke and Neelima Khairatkar-Joshi and Malini Bajpai and Ratika S Sapalya and Harshada V Surve and Girish S Gudi and Rambabu Pattem and Dayanidhi B Behera and Satyawan B Jadhav and Abraham Thomas},
  journal={Bioorganic & medicinal chemistry letters},
  year={2014},
  volume={24 9},
  pages={2073-8}
}
We report analogue-based rational design and synthesis of two novel series of polycyclic heteroarenes, pyrrolo[3,2-b]quinolines and pyrido[2,3-b]indoles, tethered to a biaryl system by a methyl-, ethyl- or propyl ether as PDE10A inhibitors. A number of analogues were prepared with variable chain length and evaluated for their ability to block PDE10A enzyme using a radiometric assay. Detailed SAR analyses revealed that compounds with an ethyl ether linker are superior in potency compared to… CONTINUE READING