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

• Published in: Molecules (Basel, Switzerland) Vol. 25; no. 6; p. 1339
• Main Authors: El Azab, Islam H, Elkanzi, Nadia A A
• Format: Journal Article
• Language: English
• Published: Switzerland MDPI AG 15-03-2020; MDPI
• Subjects: 1,2,4-triazine; 1,2,4-triazole; Anti-Infective Agents - chemical synthesis; Anti-Infective Agents - pharmacology; Antiinfectives and antibacterials; Antimicrobial activity; Antimicrobial agents; Bacteria - drug effects; Drugs; Fungi - drug effects; mannich reaction; Microbial Sensitivity Tests - methods; Mutation; n-heterocycles; NMR; Nuclear magnetic resonance; Pseudomonas aeruginosa; pyrimidine; Triazine; Triazines - chemical synthesis; Triazines - pharmacology; Triazoles - chemical synthesis; Triazoles - pharmacology; antimicrobial activity; 1,2,4-triazole; 1,2,4-triazine; pyrimidine; Mannich reaction; N-heterocycles
• ISSN: 1420-3049; 1420-3049
• DOI: 10.3390/molecules25061339

A series of 34 new pyrimido[2,1-
][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
and
-
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
ATCC 6633,
ATCC 6535,
ATCC 27853, and
ATCC 8739 (EC), and fungal strains
ATCC 10231 and
ATCC 16404.