{"title":"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","authors":"A. Hamza, A. Idris, A. Musa, A. Olorukooba","doi":"10.56892/bima.v6i03.40","DOIUrl":null,"url":null,"abstract":"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.","PeriodicalId":292938,"journal":{"name":"BIMA JOURNAL OF SCIENCE AND TECHNOLOGY (2536-6041)","volume":"2 1","pages":"0"},"PeriodicalIF":0.0000,"publicationDate":"2022-12-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"SYNTHESIS AND ANTIMALARIAL EVALUATION OF 1-(2,4- DIMETHOXYPHENYL)-3-(4-TRIFLUORO METHYL-PHENYL) PROPAN-2-ENE-1- ONE\",\"authors\":\"A. Hamza, A. Idris, A. Musa, A. Olorukooba\",\"doi\":\"10.56892/bima.v6i03.40\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"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.\",\"PeriodicalId\":292938,\"journal\":{\"name\":\"BIMA JOURNAL OF SCIENCE AND TECHNOLOGY (2536-6041)\",\"volume\":\"2 1\",\"pages\":\"0\"},\"PeriodicalIF\":0.0000,\"publicationDate\":\"2022-12-31\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"BIMA JOURNAL OF SCIENCE AND TECHNOLOGY (2536-6041)\",\"FirstCategoryId\":\"1085\",\"ListUrlMain\":\"https://doi.org/10.56892/bima.v6i03.40\",\"RegionNum\":0,\"RegionCategory\":null,\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"\",\"JCRName\":\"\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"BIMA JOURNAL OF SCIENCE AND TECHNOLOGY (2536-6041)","FirstCategoryId":"1085","ListUrlMain":"https://doi.org/10.56892/bima.v6i03.40","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"","JCRName":"","Score":null,"Total":0}
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.