Division of Image Science and Information Engineering, Pukyong National University, Busan 608 739, Republic of Korea.
Bioorg Med Chem Lett. 2010 Mar 1;20(5):1642-7. doi: 10.1016/j.bmcl.2010.01.048. Epub 2010 Jan 20.
Libraries of 1-methyl-2,4-diaryl-3-azabicyclo[3.3.1]nonan-9-ones/oximes/O-methyloximes 1-14/15-28/29-42 and 7-methyl-2,4-diaryl-3-azabicyclo[3.3.1]nonan-9-ones/oximes/O-methyloximes 43-48/49-54/55-60 were synthesized and their stereochemistry was established by 1D/2D NMR spectral and single crystal XRD studies. All the synthesized oximes and oxime ethers were screened for their in vitro antimicrobial activity against a panel of pathogenic bacteria (Bacillus subtilis, Staphylococcus aureus, Klebsiella pneumoniae and Pseudomonas aeruginosa) and fungi (Candida albicans, Candida parapsilosis, Aspergillus niger and Cryptococcus neoformans) using Gentamicin and Fluconazole as standards, respectively. From the SAR profile, the lead molecules were identified.
1-甲基-2,4-二芳基-3-氮杂双环[3.3.1]壬烷-9-酮/肟/肟醚文库 1-14/15-28/29-42 和 7-甲基-2,4-二芳基-3-氮杂双环[3.3.1]壬烷-9-酮/肟/肟醚文库 43-48/49-54/55-60 被合成，并通过 1D/2D NMR 光谱和单晶 XRD 研究确定了它们的立体化学结构。所有合成的肟和肟醚都被筛选了体外抗药性针对一组病原菌（枯草芽孢杆菌、金黄色葡萄球菌、肺炎克雷伯菌和铜绿假单胞菌）和真菌（白色念珠菌、近平滑念珠菌、黑曲霉和新型隐球菌）使用庆大霉素和氟康唑作为标准，分别。从 SAR 图谱中，确定了先导分子。
