吡唑杂合体的抗疟疾活性  

Pyrazole hybrids and their antimalarial activities

作　　者：薛华[1] 王宝君[1] 连靠奇 Xue Hua;Wang Bao-jun;Lian Kao-qi(Chemistry Teaching Group and Fundamental Medical Department,Shijiazhuang 050599;Hebei Province Key Laboratory of Environment and Human Health,Shijiazhuang 050017)

机构地区：[1]石家庄医学高等专科学校,基础医学部,医化教研室,石家庄050599 [2]河北省环境与人群健康重点实验室,石家庄050017

出　　处：《中国抗生素杂志》2020年第10期959-967,共9页Chinese Journal of Antibiotics

基　　金：河北省自然科学基金(No.H2018206122)。

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。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.

关 键 词：疟疾 吡唑 杂合体 构-效关系 

分 类 号：R978.6[医药卫生—药品]