噻唑-谷氨酸缀合物的新型尿素和硫脲衍生物作为微生物和真菌的潜在抑制剂。

Bioorganicheskaia khimiia Pub Date : 2013-11-01
A Sharma, R Suhas, S Chandan, D C Gowda
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引用次数: 0

摘要

由于有效而安全的药物的发现和开发带来了人类医疗保健的进步时代,伴随着耐药菌株的出现,人们不断需要具有新的作用机制的新型抗菌剂来对抗有害的病原体。本研究以谷氨酸和3-(1-哌嗪基)-1,2-苯并异噻唑与不同取代苯基异氰酸酯/异硫氰酸酯为原料,合成了几种n端取代脲/硫脲衍生物。元素分析、IR、1H NMR、13C NMR和质谱数据证实了新合成化合物的结构。采用琼脂孔扩散法和微量稀释法研究了其对多种人源致病菌的抑菌和抑菌活性。初步的抗菌生物试验表明,含氟和溴取代基的化合物具有良好的抗菌活性。
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Novel urea and thiourea derivatives of thiazole-glutamic acid conjugate as potential inhibitors of microbes and fungi.

Since discovery and development of effective as well as safe drugs has brought a progressive era in human healthcare that is accompanied by the appearance of drug resistant bacterial strains, there is constant need of new antibacterial agent having novel mechanisms of action to act against the harmful pathogens. In the present study, several N-terminal substituted urea/thiourea derivatives were synthesized by the reaction of glutamic acid and 3-(1-piperazinyl)-1,2-benzisothiazole with various substituted phenyl isocyanates/isothiocyanates. Elemental analysis, IR, 1H NMR, 13C NMR and mass spectral data confirmed the structure of the newly synthesized compounds. The derivatives were investigated for their antibacterial and antifungal activities against various pathogens of human origin by agar well diffusion method and microdilution method. The preliminary antimicrobial bioassay reveals that the compounds containing fluoro and bromo as substituents showed promising antimicrobial activity.

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