Raj Raghu, Biot Christophe, Carrère-Kremer Séverine, Kremer Laurent, Guérardel Yann, Gut Jiri, Rosenthal Philip J, Kumar Vipan
Department of Chemistry, Guru Nanak Dev University, Amritsar, 143005, India.
Chem Biol Drug Des. 2014 Feb;83(2):191-7. doi: 10.1111/cbdd.12225. Epub 2013 Oct 28.
A library of quinoline-β-lactam-based hybrids was synthesized and tested for their antimalarial and antitubercular activities. The present antimalarial data showed the dependence of activity on the nature of linker, N-1 substituent of the β-lactam ring as well as the length of alkyl chain. Most of the compounds are not as efficient as chloroquine in inhibiting the culture growth of Plasmodium falciparum W2 strain. Nevertheless, the synthesized hybrids showed better antitubercular activities (up to five times) compared with cephalexin (up to three times) and ethionamide.
合成了一系列基于喹啉-β-内酰胺的杂合物，并对其抗疟和抗结核活性进行了测试。目前的抗疟数据表明，活性取决于连接基的性质、β-内酰胺环的N-1取代基以及烷基链的长度。大多数化合物在抑制恶性疟原虫W2株的培养生长方面不如氯喹有效。然而，与头孢氨苄（最高三倍）和乙硫异烟胺相比，合成的杂合物显示出更好的抗结核活性（高达五倍）。
