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吡唑杂合体的抗疟疾活性
引用本文:薛华,王宝君,连靠奇.吡唑杂合体的抗疟疾活性[J].中国抗生素杂志,2020,45(10):959-967.
作者姓名:薛华  王宝君  连靠奇
摘    要:疟疾是由按蚊叮咬或输入携带疟原虫血液引起的一类高传染性疾病,其临床症状包括发热、头痛、呕吐等,如不及时治疗可能危及生命。尽管临床上使用的抗疟疾药物对疟疾的防控不可或缺,但随着长期广泛使用甚至滥用,恶性疟原虫对抗疟药物产生了不同程度的耐药性。为克服耐药性,研发新型抗疟疾药物势在必行。吡唑类化合物具有包括抗疟疾在内的多种生物活性,且某些吡唑类药物已广泛用于临床,故这类化合物引起了药物化学家的持续关注。本文将归纳吡唑杂合体在抗疟疾领域的最新研究进展,并讨论此类化合物的构-效关系。

关 键 词:疟疾  吡唑  杂合体  构-效关系  

Pyrazole hybrids and their antimalarial activities
Xue Hua,Wang Bao-jun and Lian Kao-qi.Pyrazole hybrids and their antimalarial activities[J].Chinese Journal of Antibiotics,2020,45(10):959-967.
Authors:Xue Hua  Wang Bao-jun and Lian Kao-qi
Abstract:Malaria, transmitted through the bite of an infected anopheles mosquito or by blood transfusion from a malaria infected donor, is a highly infectious disease. Malaria causes symptoms that typically include fever, vomiting, headaches, and even death in severe cases. Antimalarials are indispensable to fight against malaria, but Plasmodium falciparum has already generated resistance to almost all currently accessible antimalarials. To overcome the drug resistance, novel antimalarial agents are needed urgently. Pyrazole derivatives possess diverse biological properties including antimalarial activity, and many pyrazole-containing drugs have already used in clinics for the treatment of various diseases, and thus pyrazole derivatives play a pivotal role in the discovery of new drugs. This review covers the recent advances of pyrazole hybrids as potential antimalarial agents, and the structure-activity relationship is also discussed.
Keywords:Malaria  Pyrazole  Hybrid  Structure-activity relationship  
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