基于磺胺的非炔类LpxC抑制剂作为革兰氏阴性抗菌剂。
Sulfonamide-based non-alkyne LpxC inhibitors as Gram-negative antibacterial agents.
作者信息
Kawai Tetsuya, Kazuhiko Iwase, Takaya Noriko, Yamaguchi Yuko, Kishii Ryuta, Kohno Yasushi, Kurasaki Haruaki
机构信息
Watarase Research Center, Kyorin Pharmaceutical Co., Ltd., 1848 Nogi, Nogi-machi, Shimotsuga-gun, Tochigi 329-0114, Japan.
Watarase Research Center, Kyorin Pharmaceutical Co., Ltd., 1848 Nogi, Nogi-machi, Shimotsuga-gun, Tochigi 329-0114, Japan.
出版信息
Bioorg Med Chem Lett. 2017 Feb 15;27(4):1045-1049. doi: 10.1016/j.bmcl.2016.12.059. Epub 2016 Dec 24.
We attempted to optimize sulfonamide-based non-alkyne LpxC inhibitors by focusing on improvements in enzyme inhibitory and antibacterial activity. It was discovered that inhibitors possessing 2-aryl benzofuran as a hydrophobe exhibited good activity. In particular, compound 21 displayed impressive antibacterial activity (E. coli MIC=0.063μg/mL, K. pneumoniae MIC=0.5μg/mL, and P. aeruginosa MIC=0.5μg/mL), and is a promising lead for further exploration as an antibacterial agent.
我们试图通过专注于提高酶抑制活性和抗菌活性来优化基于磺酰胺的非炔烃类LpxC抑制剂。结果发现，具有2-芳基苯并呋喃作为疏水基团的抑制剂表现出良好的活性。特别是化合物21表现出令人印象深刻的抗菌活性（大肠杆菌的最低抑菌浓度为0.063μg/mL，肺炎克雷伯菌的最低抑菌浓度为0.5μg/mL，铜绿假单胞菌的最低抑菌浓度为0.5μg/mL），是作为抗菌剂进一步探索的有前途的先导化合物。
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