1-(2,4-二甲氧基苯基)-3-(4-三氟甲基苯基)丙烷-2-烯-1- 1的合成及抗疟评价

A. Hamza, A. Idris, A. Musa, A. Olorukooba
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引用次数: 0

摘要

疟疾是全世界最严重的健康问题之一,其治疗一直受到耐药性的影响。查尔酮是一种重要的具有抗疟疾活性的化学支架。查尔酮衍生物;采用改进的ClaisenSchmidt缩合反应合成了1(2,4二甲氧基苯基)-3-(4-三氟甲基苯基)丙烷-2-烯-1- 1(化合物P21)。利用傅里叶变换红外光谱(FT-IR)、质子和碳-13核磁共振光谱(NMR)以及质谱(MS)确定了化合物P21的结构。采用治疗模型对感染伯氏疟原虫的小鼠体内抗疟活性进行了筛选。在治疗试验中,化合物P21表现出与氯喹(5 mg kg-1)在175mg kg-1剂量下相当的活性(66%)(p<0.05)。这表明化合物P21是一种很有前途的抗疟化合物,值得进一步优化和评价。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
SYNTHESIS AND ANTIMALARIAL EVALUATION OF 1-(2,4- DIMETHOXYPHENYL)-3-(4-TRIFLUORO METHYL-PHENYL) PROPAN-2-ENE-1- ONE
Malaria is one of the most serious health problems worldwide and Its treatment has been compromised by drug resistance. Chalcones represent an important chemical scaffold with promising antimalarial activity. A chalcone derivative; 1(2,4dimethoxyphenyl)-3-(4-trifluoro methyl-phenyl) propan-2-ene-1-one (Compound P21) was synthesized by modified ClaisenSchmidt condensation reaction. The structure of compound P21 was established using Fourier transform infrared (FT-IR), proton and carbon-13 nuclear magnetic resonance (NMR) spectroscopy, and also mass spectrometry (MS). The compound was screened for in-vivo antimalarial activity in mice infected with P berghii parasite, using curative model. Compound P21 displayed appreciable activity (66% parasitaemia suppression) comparable to that of chloroquine (5 mg kg-1) at a dose of 175mg kg-1 in the curative test (p<0.05). The present finding suggests that compound P21 is a promising antimalarial compound and is a candidate for further optimization and evaluation.
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