Anthem Biosciences Pvt. Ltd., 49 Bommasandra Industrial Area, Bommasandra, Bangalore 560099, Karnataka, India.
Eur J Med Chem. 2010 Mar;45(3):957-66. doi: 10.1016/j.ejmech.2009.11.036. Epub 2009 Nov 26.
A new class of fused oxazoloquinoline derivatives was synthesized starting from 2-bromo-1-phenylethanones 1a-b through multi-step reactions. The newly synthesized compounds were evaluated for their in vitro antibacterial against Escherichia coli (ATTC-25922), Staphylococcus aureus (ATTC-25923), Pseudomonas aeruginosa (ATCC-27853) and Klebsiella pneumoniae (recultured) and antituberculosis activity against Mycobacterium tuberculosis H37Rv (ATCC 27294). Preliminary results indicated that most of the compounds demonstrated very good antibacterial and antituberculosis activities which are comparable with the first line drugs. Compounds 6a, 6c, 6g, 6j, 6k and 6n emerged as the lead antitubercular agents with MIC, 1 microg/mL and 99% bacterial inhibition while eight compounds, viz., 5a, 15k, 6a, 6c, 6g, 6j, 6k and 6n were found to be more potent than INH (MIC: 1.5 microg/mL) with MIC 1 microg/mL.
从 2-溴-1-苯乙酮 1a-b 出发，通过多步反应合成了一类新型的稠合恶唑并喹啉衍生物。对新合成的化合物进行了体外抗菌活性评价，包括对大肠杆菌（ATTC-25922）、金黄色葡萄球菌（ATTC-25923）、铜绿假单胞菌（再培养）和结核分枝杆菌 H37Rv（ATCC 27294）的抑制作用。初步结果表明，大多数化合物表现出很好的抗菌和抗结核活性，与一线药物相当。化合物 6a、6c、6g、6j、6k 和 6n 作为抗结核先导化合物，MIC 为 1μg/mL，细菌抑制率为 99%，而有 8 种化合物，即 5a、15k、6a、6c、6g、6j、6k 和 6n 的 MIC 为 1μg/mL，比 INH（MIC：1.5μg/mL）更有效。
