Discovering potent drug candidates requires new antimalarial targets.For this reason,antimalarial drug researchers focus on developing new drug candidates on promising targets.In the identification of these targets,a ...Discovering potent drug candidates requires new antimalarial targets.For this reason,antimalarial drug researchers focus on developing new drug candidates on promising targets.In the identification of these targets,a basic understanding of the metabolism and biochemical processes of malaria parasites such as Plasmodium falciparum can prove invaluable.However,malarial resistant parasites are becoming more and more significant issues as antimalarial medications progress.Antimalarial drugs are becoming increasingly resistant,thus the search for new molecules is very important task.Artemisinin based combination therapies are becoming more popular for treating malaria.This will ultimately lead to the selection of resistance due to their extensive and indiscriminate deployment.Alternative artemisinin-based combination therapies are therefore required.There is an interest in finding suitable antimalarial compounds based on their potential effectiveness against malaria.The potential activity of 1,3,4 oxadiazole analogues against malarial infections is a major draw of the search for suitable antimalarial compounds.This review identifies existing antimalarial drugs that have own therapeutic effects and evaluating their feasibility for developing novel synthetic antimalarial derivatives.展开更多
Background:Alzheimer’s disease affects millions of people worldwide,and one of its major characteristics is the accumulation of extracellular Aβpeptides in the human brain,leading to neuronal death and resulting in ...Background:Alzheimer’s disease affects millions of people worldwide,and one of its major characteristics is the accumulation of extracellular Aβpeptides in the human brain,leading to neuronal death and resulting in memory deficits,disorientation,and inappropriate behaviour.Objective and Methodology:This review study aims to develop new molecular targets for major depression-associated cognitive dysfunction and determine the mechanisms of action of 1,3,4-oxadiazole-based drug candidates.It encourages scientists to develop and synthesize drugs with low side effects to treat Alzheimer’s disease.Furthermore,the drug has shown significant improvement in memory function among dementia patients,which is due to the increased production of acetylcholine in the brain.These derivatives show a high affinity to amyloid plaques,which are thought to cause cognitive damage in patients with Alzheimer’s disease.This review study emphasizes newly developed inhibitors of amyloid deposition using the enzymeα-secretase,which cleaves amyloid precursor protein into smaller fragments that are toxic to neurons.1,3,4-Oxadiazole compounds have demonstrated no significant toxicity to the central nervous system.The antioxidant properties of 1,3,4-oxadiazoles can reduce free radicals,which play an active role in cell damage and disease.Conclusion:This review aims to provide readers with an overview of the current state of knowledge about oxadiazole-related drugs,emphasizing their biological importance.Key aspects related to the discovery and development of these drug candidates are discussed in detail,including information on their structure,biological activity,chemistry,and pharmacological properties.In addition,different derivatives discovered for Alzheimer’s disease to enhance the therapeutic efficiency of oxadiazole drugs have been comprehensively discussed in this review.展开更多
本文报道1-(5-二茂铁基-1,3,4-噻二唑-2-基)哌啶-2-酮(1)的合成。首先,在乙酸催化下,二茂铁甲醛(2)和氨基硫脲(3)反应得到二茂铁亚胺基硫脲衍生物(4)。然后,在三氯化铁作用下,中间体4发生关环反应得到5-二茂铁基-1,3,4-噻二唑-2-胺(5)...本文报道1-(5-二茂铁基-1,3,4-噻二唑-2-基)哌啶-2-酮(1)的合成。首先,在乙酸催化下,二茂铁甲醛(2)和氨基硫脲(3)反应得到二茂铁亚胺基硫脲衍生物(4)。然后,在三氯化铁作用下,中间体4发生关环反应得到5-二茂铁基-1,3,4-噻二唑-2-胺(5)。中间体5再与5-溴戊酰氯(6)发生N-酰基化反应得到5-溴-N-(5-二茂铁基-1,3,4-噻二唑-2-基)戊酰胺(7)。最后,在碱性条件下,中间体7发生分子内关环反应得到目标化合物(1)。中间体及产物结构经1 H NMR、13 C NMR和ESI-MS表征,产物1结构进一步通过X-单晶衍射确证。然后分别考察了中间体5及产物1收率的主要影响因素,确定中间体5合成的适宜条件为:三氯化铁的用量为n(三氯化铁)∶n(中间体4)=4∶1,反应温度80℃,反应时间为15 h,在该条件下,中间体5的收率达到61.9%;确定产物1合成的适宜条件为:反应溶剂为二氧六环,物料比为n(DIEA)∶n(6)∶(5)=3.0∶1.2∶1.0、反应温度为80℃,反应时间为4 h,在该条件下,产物1收率达到68.4%。展开更多
文摘Discovering potent drug candidates requires new antimalarial targets.For this reason,antimalarial drug researchers focus on developing new drug candidates on promising targets.In the identification of these targets,a basic understanding of the metabolism and biochemical processes of malaria parasites such as Plasmodium falciparum can prove invaluable.However,malarial resistant parasites are becoming more and more significant issues as antimalarial medications progress.Antimalarial drugs are becoming increasingly resistant,thus the search for new molecules is very important task.Artemisinin based combination therapies are becoming more popular for treating malaria.This will ultimately lead to the selection of resistance due to their extensive and indiscriminate deployment.Alternative artemisinin-based combination therapies are therefore required.There is an interest in finding suitable antimalarial compounds based on their potential effectiveness against malaria.The potential activity of 1,3,4 oxadiazole analogues against malarial infections is a major draw of the search for suitable antimalarial compounds.This review identifies existing antimalarial drugs that have own therapeutic effects and evaluating their feasibility for developing novel synthetic antimalarial derivatives.
文摘Background:Alzheimer’s disease affects millions of people worldwide,and one of its major characteristics is the accumulation of extracellular Aβpeptides in the human brain,leading to neuronal death and resulting in memory deficits,disorientation,and inappropriate behaviour.Objective and Methodology:This review study aims to develop new molecular targets for major depression-associated cognitive dysfunction and determine the mechanisms of action of 1,3,4-oxadiazole-based drug candidates.It encourages scientists to develop and synthesize drugs with low side effects to treat Alzheimer’s disease.Furthermore,the drug has shown significant improvement in memory function among dementia patients,which is due to the increased production of acetylcholine in the brain.These derivatives show a high affinity to amyloid plaques,which are thought to cause cognitive damage in patients with Alzheimer’s disease.This review study emphasizes newly developed inhibitors of amyloid deposition using the enzymeα-secretase,which cleaves amyloid precursor protein into smaller fragments that are toxic to neurons.1,3,4-Oxadiazole compounds have demonstrated no significant toxicity to the central nervous system.The antioxidant properties of 1,3,4-oxadiazoles can reduce free radicals,which play an active role in cell damage and disease.Conclusion:This review aims to provide readers with an overview of the current state of knowledge about oxadiazole-related drugs,emphasizing their biological importance.Key aspects related to the discovery and development of these drug candidates are discussed in detail,including information on their structure,biological activity,chemistry,and pharmacological properties.In addition,different derivatives discovered for Alzheimer’s disease to enhance the therapeutic efficiency of oxadiazole drugs have been comprehensively discussed in this review.
文摘本文报道1-(5-二茂铁基-1,3,4-噻二唑-2-基)哌啶-2-酮(1)的合成。首先,在乙酸催化下,二茂铁甲醛(2)和氨基硫脲(3)反应得到二茂铁亚胺基硫脲衍生物(4)。然后,在三氯化铁作用下,中间体4发生关环反应得到5-二茂铁基-1,3,4-噻二唑-2-胺(5)。中间体5再与5-溴戊酰氯(6)发生N-酰基化反应得到5-溴-N-(5-二茂铁基-1,3,4-噻二唑-2-基)戊酰胺(7)。最后,在碱性条件下,中间体7发生分子内关环反应得到目标化合物(1)。中间体及产物结构经1 H NMR、13 C NMR和ESI-MS表征,产物1结构进一步通过X-单晶衍射确证。然后分别考察了中间体5及产物1收率的主要影响因素,确定中间体5合成的适宜条件为:三氯化铁的用量为n(三氯化铁)∶n(中间体4)=4∶1,反应温度80℃,反应时间为15 h,在该条件下,中间体5的收率达到61.9%;确定产物1合成的适宜条件为:反应溶剂为二氧六环,物料比为n(DIEA)∶n(6)∶(5)=3.0∶1.2∶1.0、反应温度为80℃,反应时间为4 h,在该条件下,产物1收率达到68.4%。
