期刊
JOURNAL OF MICROBIOLOGICAL METHODS
卷 163, 期 -, 页码 -出版社
ELSEVIER
DOI: 10.1016/j.mimet.2019.105648
关键词
Antibacterial activity; Bacteria; Pyrimidine compounds; 1,5-benzodiazepine; Domino approach
资金
- MHRD, New Delhi, Under Training and Research in Frontier Areas of Science and Technology (FAST) Scheme
- Department of Science and Technology (DST), New Delhi under their CURIE (Consolidation of University Research for Innovation and Excellence in Women Universities) Scheme
A new series of pyrimidine (8, 14, 18 and 23) embellished analogues of 1,5-benzodiazepines were synthesized by the one-pot domino approach using the catalyst DABCO (1,4-diazabicyclo [2.2.2]octane). For each compound synthesized, anti-microbial efficacy was determined using broth microdilution assay and half maximal inhibitory concentration (IC50). Furthermore, FESEM (Field emission scanning electron microscope) studies were also carried out to observe the effect of the structure of test compounds on the morphology of both Gram-positive (S. aureus) and Gram-negative (E. coli) cell walls. The leakage of nucleotides and their integral components from compromised bacterial cells was assessed by plotting the optical density (OD) with respect to time of exposure at 320 nm. Anti-bacterial studies revealed that compound 23 was most active against targeted bacterial species. Results of the antibacterial study indicated that all the test compounds possess significant antibacterial potential against targeted bacterial strains. Amongst all, in the FE-SEM study, compound 23 caused marked alteration in bacterial cell morphology and resulted in maximum leakage of cell nucleotides in bacterial strains as compared to controls. Further efforts are required to establish their efficacy as antibacterial agents in clinical management.
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