Sharma A, Suhas R, Chandan S, Gowda D C
Bioorg Khim. 2013 Nov-Dec;39(6):736-44.
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.
由于有效且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，但同时伴随着耐药细菌菌株的出现，因此一直需要具有新型作用机制的新型抗菌剂来对抗有害病原体。在本研究中，通过谷氨酸和3-(1-哌嗪基)-1,2-苯并异噻唑与各种取代的苯基异氰酸酯/异硫氰酸酯反应合成了几种N-末端取代的脲/硫脲衍生物。元素分析、红外光谱、1H核磁共振、13C核磁共振和质谱数据证实了新合成化合物的结构。通过琼脂孔扩散法和微量稀释法研究了这些衍生物对各种人类源病原体的抗菌和抗真菌活性。初步抗菌生物测定表明，含有氟和溴作为取代基的化合物显示出有前景的抗菌活性。
