Synthesis, Characterization and Antimicrobial Activity of Novel Pharmacophores Incorporating Imidazoline-Oxazoline Scaffold

被引:11
作者
Barakat, Assem [1 ,2 ]
Al-Majid, Abdullah Mohammed [1 ]
Al-Qahatany, Faisal M. [1 ]
Islam, Mohammad Shahidul [1 ]
Al-Agamy, Mohamed H. M. [3 ,4 ]
机构
[1] King Saud Univ, Dept Chem, Coll Sci, Riyadh 11451, Saudi Arabia
[2] Univ Alexandria, Fac Sci, Dept Chem, Alexandria 21321, Egypt
[3] Al Azhar Univ, Fac Pharm, Dept Microbiol & Immunol, Cairo, Egypt
[4] King Saud Univ, Div Microbiol, Dept Pharmaceut, Coll Pharm, Riyadh 11451, Saudi Arabia
关键词
Imidazoline; Oxazoline; Antimicrobial activity; FRIEDEL-CRAFTS ALKYLATION; CATALYTIC ENANTIOSELECTIVE SYNTHESIS; ASYMMETRIC CATALYSIS; BIS-OXAZOLINE; ARYLID-BOX; ISBUT-BOX; LIGANDS; NITROALKENES; INDOLES; FAMILY;
D O I
10.5012/bkcs.2014.35.2.562
中图分类号
O6 [化学];
学科分类号
070301 [无机化学];
摘要
In this work, synthesis, characterization and antimicrobial activity of series of imidazolines-oxazolines scaffolds 5a-f and 10a-d have been investigated. All the imidazolines-oxazolines derivatives were prepared from acid derivatives 1 and 6a-c, and enantiomerically pure (S)-2-amino-3-methyl-1-butanol in four steps with excellent optical purity. The structures of all newly synthesized compounds have been elucidated by H-1, C-13 NMR, GCMS, and IR spectrometry. Their purity was continued using elemental analysis. Some newly synthesized compounds were examined to in-vitro antimicrobial activity. Among the prepared products 10d was found to exhibits the most active against all tested bacteria and fungi with minimal inhibitory concentration (MIC) ranged between 21.9 and 42.6 mu g/mL.
引用
收藏
页码:562 / 568
页数:7
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