Discovery of 6,7-dihydro-3H-pyrano[4,3-c]isoxazol-3-ones as a new class of pathogen specific anti-leptospiral agents

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• 作者：Andivelu Ilangovan^a ; ^{ilangovanbdu@yahoo.com} ; Palaniappan Sakthivel^a ; Karikalacholan Sivasankari^b ; Charles Solomon Akino Mercy^b ; Kalimuthusamy Natarajaseenivasan^b
• 关键词：5-Carboalkoxy-2 ; 3-dihydropyranone ; 6 ; 7-Dihydro-3H-pyrano[4 ; 3-c]isoxazol-3-one ; Anti-leptospiral ; Pathogen-specific ; LipL32
• 刊名：European Journal of Medicinal Chemistry
• 出版年：2017
• 出版时间：5 January 2017
• 年：2017
• 卷：125
• 期：Complete
• 页码：29-40
• 全文大小：2728 K
• 卷排序：125

文摘

Pyrano[4,3-c]isoxazol-3-ones are found to be a new class of anti-leptospiral agents. Compounds 10g shows activity at concentration as low as 62.5 μg/mL. Pathogen specific In vitro activity: 12 pathogens and 1 non pathogen screened. In vivo: Inhibits leptospires in Cy-BALB/c mice by clearing renal colonization. In silico: Compound 10g binds with pathogen specific lipoprotein LipL32.