Journal
MEDICINAL CHEMISTRY
Volume 17, Issue 7, Pages 707-723Publisher
BENTHAM SCIENCE PUBL LTD
DOI: 10.2174/1573406416666200406130047
Keywords
Visnagenone; khellinone; hydrazide; benzylidene; furoquinazolinones; antimicrobial activity; 1; 2; 4-triazolopyrimidine
Categories
Ask authors/readers for more resources
This study successfully synthesized a variety of new compounds with potential antimicrobial activity, confirmed their structures through various methods, and evaluated their antimicrobial activity in vitro. The derivatives of 1, 2, 4-triazolopyrimidofuroquinazolin-5-one showed the most efficient antimicrobial activities compared to standard drugs.
Background: Previous and recent scientific research has shown that triazolopyrimidine and furochromones have a wide range of pharmacological activities for the treatment of numerous diseases, including anticancer, antiviral, anti-depressant, anti-microbial, anti-inflammatory, and analgesic activities. Objective: Preparation of new drugs derived from a natural furochromones as (1-hydrazinyl or methylthio),-furopyrimidoquinazolinone, 1, 2, 4-triazolopyrimidofuroquinazolin-5-one, and quinazoline-pyrimidofuro- quinazoline-8, 10-dione and the study of their biological activity as antimicrobial agents. Method: A series of novel N'-furopyrimidoquinazoline-hydrazide; 1, 2, 4-triazolopyrimidofuroquinazolin-5-one; furopyrimidoquinazolin-3-one and quinazoline-pyrimidofuroquinazoline-8, 10dione derivatives were synthesized from substituted (methylthio)-furopyrimidoquinazolinone (3ab) and 1-hydrazinyl-furopyrimido- quinazolinone (4a-b) as the starting material. Results: All compounds were synthesized in good yields (71-95%) in a gradually efficient system under mild condition and some of the procedures were used such as microwave oven. The new compounds have been confirmed by means of different spectroscopic methods such as IR, 1D and 2D -NMR techniques and mass spectrum. The in vitro 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.
Authors
I am an author on this paper
Click your name to claim this paper and add it to your profile.
Reviews
Recommended
No Data Available