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.
Letters in Drug Design & Discovery
Title:Ultrasound Assisted Faster and Milder Approach to 6H-pyrido[1,2-a] quinazolin-6-imine Derivatives as Potential Inhibitors of PDE4
Volume: 14 Issue: 10
Author(s): A. S. G. Prasad, T. Bhaskara Rao, D. Rambabu, Mandava V. Basaveswara Rao*Manojit Pal*
Affiliation:
- Department of Chemistry, Krishna University, Machilipatnam-521001, Andhra Pradesh,India
- Dr. Reddy’s Institute of Life Sciences, University of Hyderabad Campus, Gachibowli, Hyderabad 500 046,India
Keywords: Quinazolinimine, ultrasound, pinner reaction, PDE4, bioactive agents, potential inhibitors.
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.Export Options
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Cite this article as:
Prasad A. S. G. , Rao T. Bhaskara , Rambabu D. , Basaveswara Rao V. Mandava *, Pal Manojit *, Ultrasound Assisted Faster and Milder Approach to 6H-pyrido[1,2-a] quinazolin-6-imine Derivatives as Potential Inhibitors of PDE4, Letters in Drug Design & Discovery 2017; 14 (10) . https://dx.doi.org/10.2174/1570180814666170317125519
DOI https://dx.doi.org/10.2174/1570180814666170317125519 |
Print ISSN 1570-1808 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-628X |
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