Differential characterization using readily accessible NMR experiments of novel N- and O-alkylated quinolin-4-ol, 1,5-naphthyridin-4-ol and quinazolin-4-ol derivatives with antimycobacterial activity

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• 作者：Eleni Pitta^a ; Olga Balabon^a ; Maciej K. Rogacki^a ; Jes&uacute ; s G&oacute ; mez^b ; Fraser Cunningham^b ; Jurgen Joosens^a ; Koen Augustyns^a ; Pieter van der Veken^a ; ^{pieter.vanderveken@uantwerpen.be} ; Robert Bates^b ; ^{robert.h.bates@gsk.com}
• 关键词：Quinolinol ; Naphthyridinol ; Quinazolinol ; Tuberculosis ; Alkylation ; Regioselectivity ; NMR
• 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：890-901
• 全文大小：1088 K
• 卷排序：125

文摘

Azaheterocyclic analogues of quinoloxyacetamide antimycobacterials are reported. Potent antimycobacterial scaffolds were identified. Unambiguous structure determination was carried out by 13C-NMR, HSQC/HMBC and NOE. NMR methodology can be applied generally for ambident heterocyclic nucleophiles.