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

Author(s): A. S. G. Prasad, T. Bhaskara Rao, D. Rambabu, Mandava V. Basaveswara Rao*, Manojit Pal*.

Journal Name: Letters in Drug Design & Discovery

Volume 14 , Issue 10 , 2017

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Graphical Abstract:


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.

Keywords: Quinazolinimine, ultrasound, pinner reaction, PDE4, bioactive agents, potential inhibitors.

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Article Details

Year: 2017
Page: [1184 - 1194]
Pages: 11
DOI: 10.2174/1570180814666170317125519
Price: $58

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