School of Studies in Chemistry, Jiwaji University, Gwalior 474011, Madhya Pradesh, India.
Eur J Med Chem. 2012 Aug;54:366-78. doi: 10.1016/j.ejmech.2012.05.020. Epub 2012 May 22.
A novel, one-pot, simple, efficient procedure for 4H-pyrimido[2,1-b]benzothiazole (4a-h), pyrazole (6a-d) and benzylidene (7a-d) derivatives of curcumin under solvent and solvent free conditions in microwave with good yield is have been synthesized. The synthesized compounds were evaluated for their antibacterial activity against gram-positive and gram-negative bacteria viz. Staphylococcus aureus, Pseudomonas aeruginosa, Salmonella typhi, Escherichia coli, Bacillus cereus and Providencia rettgeri and antifungal activity against fungi viz Aspergillus niger, Aspergillus fumigates, Aspergillus flavus. Detailed mechanistic study shows reaction proceeds through Knoevenagel type intermediate 3a which has been suggested as key intermediate for reaction (Fig. 3).
在微波溶剂和无溶剂条件下，通过一种新颖的、一锅法、简单高效的方法，以良好的产率合成了新型的 4H-嘧啶并[2,1-b]苯并噻唑（4a-h）、吡唑（6a-d）和姜黄素的亚苄基衍生物。合成的化合物进行了抗菌活性测试，分别针对革兰氏阳性菌和革兰氏阴性菌，包括金黄色葡萄球菌、铜绿假单胞菌、伤寒沙门氏菌、大肠杆菌、蜡样芽孢杆菌和雷氏普罗威登斯菌，以及抗真菌活性测试，包括黑曲霉、烟曲霉和黄曲霉。详细的机理研究表明，反应通过 Knoevenagel 型中间体 3a 进行，该中间体被认为是反应的关键中间体（图 3）。
