Synthesis and evaluation of novel spiro derivatives for pyrrolopyrimidines as anti-hyperglycemia promising compounds

Abstract

Pyrrolopyrimidin-4-ylidene-malononitriles IIa–d were prepared as important intermediates for preparation of a new series of spiro-pyrrolopyrimidines. These intermediates undergo cyclisation via reaction with acetylacetone, guanidine hydrochloride or hydrazine hydrate. Elemental and spectroscopic evidences for the structures of these compounds are presented. The final compounds have been monitored for in vivo anti-hyperglycemic activity, compared with Amaryl as standard drug. Among 12 tested compounds, both spiro (pyrano IIIb and pyrazlo Va) derivatives exhibit promising anti-hyperglycemic activity.

Keywords:

• Spiropyrimidines
• pyrrolopyrimidines
• anti-hyperglycemic assay

Acknowledgements

We like to convey our grateful thanks for Mossad Said Mohamed (Professor of Pharmaceutical Organic Chemistry) and the staff members of Faculty of Pharmacy, Helwan University for their inspiration and support.

Disclosure statement

We wish to declare that there are no recognised conflicts of interest connected with this publication and there has been no remarkable financial funding for this work that could have influenced its outcome. We authorise that the manuscript has been read and approved by all named authors, and that there are no other persons who fulfilled the standards for authorship but are not listed.