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Synthesis and Antimicrobial Activity of Novel 1, 2, 4-Triazolopyrimidofuro- quinazolinones from Natural Furochromones (Visnagenone and Khellinone)

Author(s):

Ameen Ali Abu-Hashem*, Hoda A. R. Hussein and Ahmed S. Aly   Pages 1 - 17 ( 17 )

Abstract:


Background: Previous and recent scientific research has shown that triazolopyrimidine and furochromones have a wide range of pharmacological activities in the treatment of numerous diseases, including anticancer, antiviral, anti-depressant, antimicrobial, anti-inflammatory, and analgesic activities.

Objective: Preparation of new drugs used as antimicrobial activities derived from a natural furochromones as (1- hydrazinyl or methylthio),-furopyrimidoquinazolinone, 1, 2, 4-triazolopyrimidofuroquinazolin-5-one, and quinazolinepyrimidofuro- quinazoline-8, 10-dione and study of their biological activity as antimicrobial.

Method: A series of novel N’-furopyrimidoquinazoline-hydrazide; 1, 2, 4-triazolopyrimidofuroquinazolin-5-one; furopyrimidoquinazolin-3-one and quinazoline-pyrimidofuroquinazoline-8, 10-dione derivatives were synthesized from substituted (methylthio)-furopyrimidoquinazolinone (3a-b) and 1-hydrazinyl-furopyrimidoquinazolinone (4a-b) as the starting material.

Results: All compounds were synthesized in good yields (71-95%) in a gradually efficient system under the mild condition and some of the procedures were used a microwave oven. The new compounds have been confirmed by means of different spectroscopic ways such as IR, 1D and 2D -NMR techniques and mass spectrum. The in vitro to antimicrobial activities were evaluated for the prepared compounds using many types of bacteria (Gram positive and Gram negative) and fungi.

Conclusion: 1, 2, 4-triazolopyrimidofuroquinazolin-5-one derivatives (10a-f, 8a-b, 7a-b and 6a-d) showed the most efficient antimicrobial activities compared with the cefotaxime sodium and nystatin as standard drugs.

Keywords:

visnagenone, khellinone, hydrazide, 1, 2, 4-triazolopyrimidine, benzylidene, furoquinazolinones, antimicrobial activity.

Affiliation:

Photochemistry Department (Heterocyclic Unit), National Research Center, 12622 Dokki, Giza, Photochemistry Department (Heterocyclic Unit), National Research Center, 12622 Dokki, Giza, Photochemistry Department (Heterocyclic Unit), National Research Center, 12622 Dokki, Giza



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