当前位置: X-MOL 学术Phosphorus Sulfur Silicon Relat. Elem. › 论文详情
Our official English website, www.x-mol.net, welcomes your feedback! (Note: you will need to create a separate account there.)
2-(Benzo[d]thiazol-2-yl) phenyl-4-nitrophenyl alkyl/aryl substituted phosphramidates: Synthesis, characterization and antimicrobial activity evaluation
Phosphorus, Sulfur, and Silicon and the Related Elements ( IF 1.4 ) Pub Date : 2017-12-06 , DOI: 10.1080/10426507.2017.1392960
S. Munichandra Reddy 1 , D. Subba Rao 2 , K. Madhu 2 , Ch. Subramanyam 3 , P. Gnana Kumari 1 , C. Naga Raju 4
Affiliation  

GRAPHICAL ABSTRACT ABSTRACT A series of new 2-(benzo[d]thiazol-2-yl) phenyl-4-nitrophenyl alkyl/aryl substituted phosphoramidate derivatives (7a-j) of biological interest are synthesized in two steps via an in situ process without the isolation of the intermediate. 2-(Benzo[d]thiazol-2-yl) phenol (3) was treated with 4-nitrophenyl phosphorodichloridate(4) to obtain the monochloro intermediate, 2-(benzo[d]thiazol-2-yl)phenyl (4-nitrophenyl) phosphorochloridate(5). It was subsequently reacted with various amines, 6(a-j) to afford the desired title products. IR, NMR (1H, 13C and 31P), mass spectral and elemental analysis are used to characterize the structures of the newly synthesized compounds. The antibacterial and antifungal activities are determined by the growth of inhibition of bacteria and fungi of the title compounds at two concentrations, 50 and 100 µg/mL, and minimum inhibitory concentrations to the active compounds. The compounds 7e, 7f and 7j exhibited promising inhibition activity against bacterial strains and 7c, 7e and 7i against A. niger and C. albicans and MIC values are in the range of 10.0–15.0 µg/mL.

中文翻译:

2-(Benzo[d]thiazol-2-yl) 苯基-4-硝基苯基烷基/芳基取代的磷酰胺:合成、表征和抗菌活性评估

图形摘要摘要 一系列具有生物学意义的新型 2-(苯并[d] 噻唑-2-基) 苯基-4-硝基苯基烷基/芳基取代的氨基磷酸酯衍生物 (7a-j) 是通过原位工艺分两步合成的,无需中间体的分离。2-(苯并[d]噻唑-2-基)苯酚(3)用4-硝基苯基二氯化磷(4)处理,得到一氯中间体2-(苯并[d]噻唑-2-基)苯基(4-硝基苯基) 磷酰氯 (5)。随后将其与各种胺 6(aj) 反应,得到所需的标题产物。IR、NMR(1H、13C 和 31P)、质谱和元素分析用于表征新合成化合物的结构。抗菌和抗真菌活性由两种浓度的标题化合物对细菌和真菌的抑制作用决定,50 和 100 µg/mL,以及对活性化合物的最小抑制浓度。化合物 7e、7f 和 7j 对细菌菌株表现出良好的抑制活性,7c、7e 和 7i 对黑曲霉和白色念珠菌具有良好的抑制活性,MIC 值在 10.0-15.0 µg/mL 的范围内。
更新日期:2017-12-06
down
wechat
bug