Tiwari Rakesh Kumar, Singh Devender, Singh Jaspal, Chhillar Anil Kumar, Chandra Ramesh, Verma Akhilesh Kumar
Synthetic Organic Chemistry Research Laboratory, Dr. B.R. Ambedkar Center for Biomedical Research, University of Delhi, Delhi 110007, India.
Eur J Med Chem. 2006 Jan;41(1):40-9. doi: 10.1016/j.ejmech.2005.10.010. Epub 2005 Dec 13.
Some new substituted-tetrahydroisoquinoline derivatives were synthesized and evaluated for their in vitro antimicrobial activities against the standard Gram positive and Gram negative strains: Staphylococcus aureus (ATCC 25923), S. epidermidis (WHO-6), Escherichia coli (ATCC 25922), Pseudomonas aeruginosa (ATCC 27853), 1-aryl-6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline 4a-c proved to be effective with MIC 3.5-20 (microg ml(-1)). Quantitative structure activity relationship (QSAR) studies with multiple linear regression analysis were applied to find correlation between different calculated molecular descriptors of the synthesized compounds and biological activity.
合成了一些新的取代四氢异喹啉衍生物，并对其针对标准革兰氏阳性和革兰氏阴性菌株的体外抗菌活性进行了评估：金黄色葡萄球菌（ATCC 25923）、表皮葡萄球菌（WHO-6）、大肠杆菌（ATCC 25922）、铜绿假单胞菌（ATCC 27853），1-芳基-6,7-二甲氧基-1,2,3,4-四氢异喹啉4a-c被证明具有有效性，其最低抑菌浓度（MIC）为3.5 - 20（微克/毫升）。采用多元线性回归分析进行定量构效关系（QSAR）研究，以找出合成化合物的不同计算分子描述符与生物活性之间的相关性。
