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首页> 外文会议>International Conference on Applied Sciences >Structure-based design synthesis of functionalized 3-(5-(s-phenyl)-4H-pyrazol-3-yl)-2H-chromen-2-one motifs and indigenous plant extracts and their antimalarial potential
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Structure-based design synthesis of functionalized 3-(5-(s-phenyl)-4H-pyrazol-3-yl)-2H-chromen-2-one motifs and indigenous plant extracts and their antimalarial potential

机译：基于结构的官能化3-（5-（S-（S-（S-（S-（S-（S-（S-（S-（S-）-4H-吡唑-3-基-2-2 -ON-1 -ONIF和土着植物提取物及其抗疟疾电位的设计合成

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Resistance of the malaria parasite to conventional therapeutic agents calls for increased efforts in antimalarial drug discovery. Current efforts should be targeted at developing safe and affordable new agents to counter the spread of malaria parasites that are resistant to existing therapy. In this study, toxicological and in vivo antiplasmodial properties of 3-(5-(s-phenyl)-4H-pyrazol-3-yl)-42H-chromen-2, Mangifera indica and Tithonia diversifolia in swiss albino mice models, Musmusculus were investigated. 2H-Chromen-2-one also known as coumarin is highly privileged oxygen-containing heterocyclic entity which are present in plant kingdom as secondary metabolites. The maceration technique of crude drug extraction was employed using cold water extraction. Toxicological analysis was carried out using Lorke’s method for acute toxicity testing while the chemosuppressive activity was carried out using Peter’s four day test on early infection. We also report the synthesis of functionalized 3-(5-(s-phenyl)-4H-pyrazol-3-yl)-2H-chromen-2-one motifs via microwave assisted synthetic approach and isolation of indigenous plant extract in order to investigate their antimalarial efficacy. The condensation reaction of 3-acetylcoumarin with various benzaldehyde derivatives resulted in the formation of 3-[3-acryloyl]-2H-chromen-2-one which was subsequently reaction the hydrazine hydrate via microwave assisted hydrazinolysis to afford the targeted 3-(5-(s-phenyl)-4H-pyrazol-3-yl)-2H-chromen-2-one motifs. The chemical structures were confirmed by analytical data and spectroscopic means such as FT-IR, UV, ~1H NMR, ~(13)C NMR and DEPT-135. The microwave assisted reaction was remarkably successful and gave targeted 3-(5-(s-phenyl)-4H-pyrazol-3-yl)-2H-chromen-2-one motifs in higher yields at lesser reaction time compared to conventional heating method. The LD_(50) of the aqueous extracts of the leaves and stem bark Mangifera indica was established to be ± 707.11 mg/kg b.w., p.o. (body weight, administered orally) in mice. Tithonia diversifolia aqueous leaf extracts is non-toxic at doses as high as 1000 mg/kg while the LD_(50) of the ethanolic leaf extracts was established to be ± 707.11 mg/kg b.w., p.o. in mice. The in vivo antiplasmodial activity was studied in chloroquine-sensitive Plasmodium berghei berghei - NK65 infected mice. All the plant extracts, at the doses (100, 200 and 400 mg/kg b.w., p.o.) used, produced significant (p < 0.05), dose dependent activity (> 80% inhibition of parasitaemia at maximum dose) against the parasite in the suppressive tests. The in vitro antimalarial screening of the synthesized compounds is presently on-going and the finding will be reported in due course.
机译：疟疾寄生虫对抗疟疾药物发现加大力度常规治疗剂的呼叫阻力。当前应努力在开发安全和负担得起的新药来对付疟原虫是现有的治疗性传播为目标。在这项研究中，毒理学和体内抗疟原虫3-性质（5-（S-苯基）-4H-吡唑-3-基）-42H-色烯2，芒果和肿柄菊在瑞士白化小鼠模型，Musmusculus分别调查。 -2H-色烯-2-酮也称为香豆素是高特权含氧杂环实体其存在于植物界作为次级代谢产物。使用冷水萃取采用生药提取浸渍技术。毒理学分析进行了使用急性毒性试验Lorke的方法，而chemosuppressive活性用彼得的四大天的测试在感染早期进行。我们还报告官能3-合成（5-（S-苯基）-4H-吡唑-3-基）-2H-色烯-2-酮通过微波辅助图案土著植物提取物的合成方法和分离，以便调查他们的抗疟功效。 3-乙酰基香豆素与各种苯甲醛衍生物的缩合反应导致形成3- [3-丙烯酰基] -2H-色烯-2-酮，其为随后的反应通过微波辅助肼水合肼，得到目标的3-（5- - （S - 苯基）-4H-吡唑-3-基）-2H-色烯-2-酮基序。的化学结构进行了分析数据和光谱手段如FT-IR，UV，〜1H NMR，〜（13）C NMR和DEPT-135确认。微波辅助的反应是非常成功和都给靶向3-（5-（S-苯基）-4H-吡唑-3-基）-2H-色烯-2-酮在较小的反应时间在更高的产量的基序相对于传统的加热方法。叶的水性提取物的LD_（50）和茎皮芒果成立为±707.11毫克/ kg体重，口服（体重，口服给药）的小鼠。肿柄菊水叶提取物是在剂量高达1000毫克/公斤无毒而叶乙醇提取物的LD_（50）成立为±707.11毫克/ kg体重，口服在老鼠中。 NK65感染小鼠 - 体内抗疟原虫活性在氯喹敏感疟原虫伯氏疟原虫的研究。所有的植物提取物，在剂量（100，200和400毫克/公斤体重，口服）使用时，产生的显著（P <0.05），剂量依赖性活性（>寄生虫血症的80％抑制在最大剂量）对在寄生虫抑制试验。合成的化合物的体外筛选抗疟药是目前正在进行的和的发现将在适当的时候进行报告。

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