四氮唑杂合体在抗疟疾领域的研究进展

疟疾主要是由恶性疟原虫引起的一类可致命传染性疾病,与艾滋病、结核病一起被认为是全球最重要的三大公共卫生问题。临床上使用的抗疟疾药物如喹啉类和青蒿素类尽管对药敏型疟疾依然高度有效,但随着耐药疟疾的不断涌现和广泛传播,现有抗疟疾药物的疗效呈逐年下降之势。因此,亟需开发新型抗疟疾药物。四氮唑作为羧基的生物电子等排体可用来取代药物中的羧基以提高药物分子的脂溶性、增加药物的生物利用度和降低毒副作用,故四氮唑被认为是最具发展前景的一类化合物。本文将着重介绍近年来四氮唑杂合体在抗疟疾领域的研究进展,并讨论此类化合物的构-效关系。

Recent Advances of Tetrazole Hybrids as Potential Antimalarial Agents

Malaria,caused mainly by Plasmodium falciparum,is a serious life-threatening parasitic infectious disease.Antimalarial agents such as quinolines and artemisinin are critical for the treatment of malaria,but malaria control is extremely challenged by the emergency and widely spread of various forms of drug-resistant malaria which are resistant to almost all currently accessible antimalarial agents.Obviously,it’s imperative to develop new antimalarial drugs.Tetrazole as the bioisostere of the carboxylic acid group can instead of carboxyl group in drugs to increase the lipophilicity,improve bioavailability and reduce side effects,so tetrazole derivatives occupy an important position in the discovery of new drugs.This review covers the recent advances of tetrazole hybrids as potential antimalarial agents,and the structure-activity relationship is also discussed.