Microwave-Assisted Synthesis, Structural Characterization and Assessment of the Antibacterial Activity of Some New Aminopyridine, Pyrrolidine, Piperidine and Morpholine Acetamides

被引:13
作者
Alsamarrai, Abdulmajeed S. H. [1 ]
Abdulghani, Saba S. [1 ]
机构
[1] Univ Samarra, Coll Appl Sci, Dept Chem, Salahaldin 13-1333, Samarra, Iraq
来源
MOLECULES | 2021年 / 26卷 / 03期
关键词
acetamide; pyridine; pyrrolidine; piperidine; morpholine; antibacterial activity; heterocycles; ANTIMICROBIAL ACTIVITY; BIOLOGICAL EVALUATION; MOLECULAR DOCKING; IN-VITRO; AMIDE; DERIVATIVES; DESIGN; LEVOBUPIVACAINE;
D O I
10.3390/molecules26030533
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
A series of new acetamide derivatives 22-28 of primary and secondary amines and para-toluene sulphinate sodium salt have been synthesized under microwave irradiation and assessed in vitro for their antibacterial activity against one Gram-positive and two Gram-negative bacterial species such as S. pyogenes, E. coli, and P. mirabilis using the Mueller-Hinton Agar diffusion (well diffusion) method. The synthesized compounds with significant differences in inhibition diameters and MICs were compared with those of amoxicillin, ampicillin, cephalothin, azithromycin and doxycycline. All of the evaluated acetamide derivatives were used with varying inhibition concentrations of 6.25, 12.5, 37.5, 62.5, 87.5, 112.5 and 125 mu g/mL. The results show that the most important antibacterial properties were displayed by the synthetic compounds 22 and 24, both of bear a para-chlorophenyl moiety incorporated into the 2-position moiety of acetamide 1. The molecular structures of the new compounds were determined using the FT-IR and H-1-NMR techniques.
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页数:16
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