SeQuent Scientific Ltd., No. 120 A & B, Industrial Area, Baikampady, New Mangalore 575 011, Karnataka, India.
Eur J Med Chem. 2011 Aug;46(8):3531-6. doi: 10.1016/j.ejmech.2011.05.005. Epub 2011 May 12.
In the present study two series of novel imidazole derivatives containing substituted pyrazole moiety (3a-d and 5a-j) were synthesized. The first series were synthesized by the reaction of 3-aryl-1H-pyrazole-4-carbaldehyde thiosemicarbazones (2a-d) with DMAD and the second series by the reaction of 3-aryl-1H-pyrazole-4-carbaldehydes (1a-e) with 1,2-diketones (4a,b) in the presence of ammonium acetate. Structures of newly synthesized compounds were characterized by spectral studies. New compounds were screened for antifungal and antibacterial activities. Among the synthesized compounds, compound 3c was found to be potent antimicrobial agent. The acute oral toxicity study for the compound 3c was carried out and the experimental studies revealed that compound 3c is safe up to 3000 mg/kg and no death of animals were recorded.
在本研究中，合成了两个含有取代吡唑部分的新型咪唑衍生物系列（3a-d 和 5a-j）。第一个系列是通过 3-芳基-1H-吡唑-4-甲酰基缩氨硫脲（2a-d）与 DMAD 的反应合成的，第二个系列是通过 3-芳基-1H-吡唑-4-甲酰基（1a-e）与 1,2-二酮（4a，b）在醋酸铵存在下的反应合成的。新合成化合物的结构通过光谱研究进行了表征。新化合物被筛选出具有抗真菌和抗菌活性。在所合成的化合物中，化合物 3c 被发现是一种有效的抗菌剂。对化合物 3c 进行了急性口服毒性研究，实验研究表明，化合物 3c 在高达 3000mg/kg 的剂量下是安全的，没有动物死亡的记录。
