脲/草酰亚胺键联的β-内酰胺-7-氯喹啉轭合物的合成及体外抗疟活性评价。
Urea/oxalamide tethered β-lactam-7-chloroquinoline conjugates: synthesis and in vitro antimalarial evaluation.
机构信息
Department of Chemistry, Guru Nanak Dev University, Amritsar 143005, Punjab, India.
Department of Chemistry, Durban University of Technology, Durban 4000, South Africa.
出版信息
Eur J Med Chem. 2014 Jan;71:128-34. doi: 10.1016/j.ejmech.2013.10.079. Epub 2013 Nov 9.
The manuscript pertains to the synthesis of urea/oxalamide tethered β-lactam-7-chloroquinoline conjugates with well modulated chain lengths and their antimalarial evaluation. The results reveal the dependence of activity profiles on the N-1 substituent of the β-lactam ring, the nature of the linker as well as the length of the alkyl chain. The most potent of the tested compounds showed an IC50 of 34.97 nM against chloroquine resistant W2 strain of Plasmodium falciparum.
本文涉及到尿素/草酰亚胺键合的β-内酰胺-7-氯喹啉缀合物的合成，这些缀合物具有良好调节的链长，并对其进行了抗疟疾评估。结果表明，活性谱取决于β-内酰胺环的 N-1 取代基、连接体的性质以及烷基链的长度。在所测试的化合物中，最有效的化合物对氯喹耐药的恶性疟原虫 W2 株的 IC50 为 34.97 nM。
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