Synthesis and antibacterial activity of 3-arylaminomethyl-1-(2-oxo-2-arylethyl)-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a] azepin-1-ium bromides and aryl-(4-R1-phenyl-5,6,7,8-tetrahydro-2,2a,8a-triazacyclopenta[cd]azulen-1-ylmethyl)-amines
نویسندگان
چکیده
The aim of this work is to develop methods synthesis 3-arylaminomethyl-1-(2-oxo-2-arylethyl)-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepin-1-ium bromides and aryl-(4-R1-phenyl-5,6,7,8-tetrahydro-2,2a,8a-triazacyclopenta[cd]azulen-1-ylmethyl)-amines study their antimicrobial activity against strains gram-positive gram-negative bacteria as well yeast fungi.
 Materials methods. 1Н NMR spectra were recorded on Bruker 400 spectrometer operating at frequency MHz. Antimicrobial the compounds synthesized was evaluated by minimum inhibitory concentration (MIC) values.
 Results discussion. interaction 3-arylaminomethyl-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepines with substituted phenacyl produced novel bromides. latter when refluxed in 10 % solution NaOH gave aryl-(4-R1-phenyl-5,6,7,8-tetrahydro-2,2a,8a-triazacyclopenta[cd]azulen-1-ylmethyl)-amines. obtained allowed find derivatives which are active С. albicans S. aureus strains. Among tested 3-[(41-bromophenylamino)-methyl]-1-[2-(4-methoxyphenyl)-2-oxoethyl]-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepin-1-ium bromide 5cd appeared be more than reference drug Cefixime displayed close antibiotic Linezolid.
 Conclusions. It found out that display broad spectrum able inhibit growth both fungi. C. turned most sensitive tested, MIC range 6.2-25.0 mg/mL. Gram-negative microorganisms less 5fа derivative displaying 50.0 triazoloazepinium similar one Linezolid Fluconazole drugs pronounced Cefixime.
 Hence, data gathered evidence feasibility further properties vivo experiments aiming assessment prospects for creation new effective safe based them
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ژورنال
عنوان ژورنال: ScienceRise
سال: 2021
ISSN: ['2519-4798', '2519-478X']
DOI: https://doi.org/10.15587/2519-4852.2021.249480