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Azirine-containing dipeptides and depsipeptides: synthesis, transformations and antibacterial activity
Organic & Biomolecular Chemistry ( IF 2.9 ) Pub Date : 2020-11-05 , DOI: 10.1039/d0ob02023k Nikolai V Rostovskii 1 , Alexander N Koronatov 1 , Pavel A Sakharov 1 , Anastasiya V Agafonova 1 , Mikhail S Novikov 1 , Alexander F Khlebnikov 1 , Elizaveta V Rogacheva 2 , Liudmila A Kraeva 3
Organic & Biomolecular Chemistry ( IF 2.9 ) Pub Date : 2020-11-05 , DOI: 10.1039/d0ob02023k Nikolai V Rostovskii 1 , Alexander N Koronatov 1 , Pavel A Sakharov 1 , Anastasiya V Agafonova 1 , Mikhail S Novikov 1 , Alexander F Khlebnikov 1 , Elizaveta V Rogacheva 2 , Liudmila A Kraeva 3
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Azirine-containing dipeptides and depsipeptides with a wide range of substituents have been synthesized in high yields via the Passerini and Ugi multicomponent reactions (MCRs) using 2H-azirine-2-carboxylic acids as the acid component. The obtained MCR adducts have been transformed to lactam-fused aziridines, as well as pyrrole, imidazole, aziridine, and other derivatives, containing the dipeptide or depsipeptide moiety. The azirine-containing depsipeptides exhibit antibacterial activity against the ESKAPE pathogens, especially Gram-positive bacterial strains (E. faecium – MIC 16 μg mL−1, S. aureus – MIC 9 μg mL−1).
中文翻译：
含氮丙啶的二肽和缩酚肽：合成、转化和抗菌活性
使用 2 H-氮丙啶-2-羧酸作为酸组分，通过Passerini 和 Ugi 多组分反应 (MCR) 高产率合成了具有多种取代基的含氮丙啶二肽和缩酚酸肽。获得的MCR加合物已转化为内酰胺稠合的氮丙啶，以及含有二肽或缩酚肽部分的吡咯、咪唑、氮丙啶和其他衍生物。含氮丙啶的缩酚肽对 ESKAPE 病原体，特别是革兰氏阳性菌株（屎肠球菌– MIC 16 μg mL -1 ，金黄色葡萄球菌– MIC 9 μg mL -1 ）表现出抗菌活性。
更新日期：2020-11-12
中文翻译：
含氮丙啶的二肽和缩酚肽：合成、转化和抗菌活性
使用 2 H-氮丙啶-2-羧酸作为酸组分，通过Passerini 和 Ugi 多组分反应 (MCR) 高产率合成了具有多种取代基的含氮丙啶二肽和缩酚酸肽。获得的MCR加合物已转化为内酰胺稠合的氮丙啶，以及含有二肽或缩酚肽部分的吡咯、咪唑、氮丙啶和其他衍生物。含氮丙啶的缩酚肽对 ESKAPE 病原体，特别是革兰氏阳性菌株（屎肠球菌– MIC 16 μg mL -1 ，金黄色葡萄球菌– MIC 9 μg mL -1 ）表现出抗菌活性。
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