MICROWAVE ASSISTED SYNTHESIS AND DETERMINATION OF IN-VITRO ANTIMICROBIAL EFFICACY OF WELL CHARACTERIZED S-TRIAZINYL PIPERAZINES AND PIPERIDINES

被引:0
|
作者
Patel, Rahul V. [1 ]
Kumari, Premlata [1 ]
Chikhalia, Kishor H. [2 ]
机构
[1] SV Natl Inst Technol, Dept Appl Chem, Surat 395007, India
[2] Gujarat Univ, Sch Sci, Dept Chem, Ahmadabad 380025, Gujarat, India
来源
ACTA POLONIAE PHARMACEUTICA | 2012年 / 69卷 / 03期
关键词
2,4,6-trichloro-1,3,5-triazine; 8-hydroxyquinoline; 4-aminobenzonitrile; piperazines and piperidines; antimicrobial activity; REVERSE-TRANSCRIPTASE INHIBITORS; ANTIMALARIAL ACTIVITY; ANTIBACTERIAL ACTIVITY; AROMATIC CHELATORS; DERIVATIVES; AGENTS; FLUORINE; FLUOROQUINOLONES; RESISTANCE; CHEMISTRY;
D O I
暂无
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
An easy and convenient microwave-assisted synthesis of a library of s-triazinyl piperazines and piperidines, which, in addition to 4-aminobenzonitrile contain 8-hydroxyquinoline is described. The newly synthesized analogues were then subjected to determine their efficacy against some human pathogenic bacterial and fungal strains as 3 Gram negative bacteria (K. pneumoniae, S. typhi, P. vulgaris), I Gram positive bacteria (B. cereus) and 2 fungal species (A. clavatus, A. fumigatus) with an intent to develop novel class of antimicrobial agents. Microwave irradiation method was adopted for the final nucleophilic reactions, facilitates the condensation of piperazine and piperidine substituents to the s-triazine core. The results of bioassay showed that some of the newly synthesized s-triazines emerged as lead molecules with execellent MIC (mg/mL) values against the full array of bacterial and fungal pathogens comparable to the commercial antibiotics. The structure of final scaffolds has been affirmed on the basis of IR. H-1 NMR, C-13 NMR, F-19 NMR and elemental analyses.
引用
收藏
页码:423 / 432
页数:10
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