Synthesis of mono-, bis-spiro- and dispiro-β-lactams and evaluation of their antimalarial activities
作者:Aliasghar Jarrahpour、Edris Ebrahimi、Erik De Clercq、Véronique Sinou、Christine Latour、Lamia Djouhri Bouktab、Jean Michel Brunel
DOI:10.1016/j.tet.2011.09.041
日期:2011.11
Some new mono-, bis-spiro- and dispiro-β-lactams have been synthesized from imines derived from 9H-fluoren-9-one and a ketene derived from 9H-xanthene-9-carboxylic acid or phenoxyacetic acid by a [2+2] cycloaddition reaction in good to excellent yields varying from 45 to 83%. The biological activity of these monocyclic β-lactams was successfully investigated against Plasmodium falciparum K14 resistant
某些新的单,双-螺和双-螺-β-内酰胺是由[9 H-芴-9-一]衍生的亚胺和由9 H -carboxylic吨9-羧酸或苯氧乙酸衍生的乙烯酮合成的[ [2 + 2]环加成反应的良好至优异收率从45%到83%不等。已成功研究了这些单环β-内酰胺类抗恶性疟原虫K14抗性菌株的生物学活性,该菌株的EC 50值高达5μM。