Ultrasound Assisted Faster and Milder Approach to 6H-pyrido[ 1,2-a] quinazolin-6-imine Derivatives as Potential Inhibitors of PDE4

作者：Prasad A S G; Rao T Bhaskara; Rambabu D; Rao Mandava V Basaveswara^*; Pal Manojit^*

来源：Letters in Drug Design and Discovery, 2017, 14(10): 1184-1194.

DOI：10.2174/1570180814666170317125519

• Quinazolinimine
• ultrasound
• pinner reaction
• PDE4
• bioactive agents
• potential inhibitors

Background: The ultrasound assisted methodology has been explored first time for the quicker synthesis of 6H-pyrido[1,2-a] quinazolin-6-imine derivatives via the reaction of 2-aminopyridines and 2-fluorobenzontriles under mild conditions.
Methods: The methodology is free from the use of any transition metal catalyst and afforded the desired products in good yields. Some of the synthesized compounds were evaluated for their potential PDE4 inhibition in silico and subsequently in vitro.
Conclusion: One compound showed dose dependent inhibition of PDE4B and favorable pharmacological properties indicating potential of this scaffold for the discovery of new inhibitors of PDE4.

• 出版日期2017