A simple and efficient one-pot novel synthesis of pyrazolo[3,4-b][1,8]naphthyridine and pyrazolo[3,4-d]pyrimido[1,2-a]pyrimidine derivatives as anti-inflammatory agents

作者：Patil Priyanka T.; Warekar Poojali P.; Patil Kirti T.; Undare Santosh S.; Jamale D. K.; Vibhute S. S.; Valekar N. J.; Kolekar Govind B.; Deshmukh Madhukar B.; Anbhule Prashant. V.^*

来源：Research on Chemical Intermediates, 2018, 44(2): 1119-1130.

DOI：10.1007/s11164-017-3155-5

• Pyrazolo[3,4-b][1,8]naphthyridine derivatives
• Pyrazolo[3,4-d]pyrimido[1,2-a]pyrimidine derivatives
• In vivo anti-inflammatory activity and multicomponent reaction

An efficient one-pot synthesis of novel pyrazolo[3,4-b][1,8]naphthyridine and pyrazolo[3,4-d]pyrimido[1,2-a]pyrimidine derivatives has been investigated from the reaction of 2-amino (pyrimidine or pyridine), aromatic aldehydes and 3-methyl-1-phenyl-2-pyrazolin-5-one. All synthesized compounds were evaluated for in vivo anti-inflammatory activity using carrageenan-induced rat paw edema assay. Compounds 4a, 4e, 4g, 5a, 5b (80%) and 5c (86%) showed good to excellent results when compared with the anti-inflammatory active standard drug diclofenac Na (93%). On the basis of the structure-activity relationship, the anti-inflammatory activity of pyrazolo[3,4-d]pyrimido[1,2-a]pyrimidine derivatives has been found to be much better than pyrazolo[3,4-b][1,8]naphthyridine derivatives.

• 出版日期2018-2