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Open AccessArticle

Design, Synthesis, and Antimicrobial Evaluation of New Annelated Pyrimido[2,1-c][1,2,4]triazolo[3,4-f][1,2,4]triazines

1
Chemistry Department, Faculty of Science, Taif University, Al-Haweiah, P.O. Box 888, Taif 21974, Saudi Arabia
2
On leave from Chemistry Department, Faculty of Science, Aswan University, Aswan P.O. Box 81528, Egypt
3
Chemistry Department, College of Science, Jouf University, P.O. Box 2014, Sakaka, Saudi Arabia
*
Author to whom correspondence should be addressed.
Academic Editor: Vincenzo Piccialli
Molecules 2020, 25(6), 1339; https://doi.org/10.3390/molecules25061339
Received: 30 January 2020 / Revised: 7 March 2020 / Accepted: 13 March 2020 / Published: 15 March 2020
(This article belongs to the Special Issue Application of Organic Synthesis to Bioactive Compounds)
A series of 34 new pyrimido[2,1-c][1,2,4]triazine-3,4-diones were synthesized and fully characterized using IR, NMR, MS, and microanalytical analysis. In vitro investigation of 12 compounds of this series revealed promising antimicrobial activity of the conjugates 15a and 15fj that were tagged with electron-withdrawing groups, with sensitivities ranging from 77% to as high as 100% of the positive control. The investigation of antimicrobial activity included Bacillus subtilis ATCC 6633, Staphylococcus aureus ATCC 6535, Pseudomonas aeruginosa ATCC 27853, and Escherichia coli ATCC 8739 (EC), and fungal strains Candida albicans ATCC 10231 and Aspergillus brasiliensis ATCC 16404. View Full-Text
Keywords: Mannich reaction; 1,2,4-triazine; pyrimidine; 1,2,4-triazole; N-heterocycles; antimicrobial activity Mannich reaction; 1,2,4-triazine; pyrimidine; 1,2,4-triazole; N-heterocycles; antimicrobial activity
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MDPI and ACS Style

El Azab, I.H.; Elkanzi, N.A. Design, Synthesis, and Antimicrobial Evaluation of New Annelated Pyrimido[2,1-c][1,2,4]triazolo[3,4-f][1,2,4]triazines. Molecules 2020, 25, 1339.

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