86404-63-9Relevant articles and documents
Design, synthesis and antitrypanosomal activity of some nitrofurazone 1,2,4-triazolic bioisosteric analogues
Silva, Fredson T.,Franco, Caio H.,Favaro, Denize C.,Freitas-Junior, Lucio H.,Moraes, Carolina B.,Ferreira, Elizabeth I.
, p. 553 - 560 (2016)
Chagas disease, caused by Trypanosoma cruzi, is a parasitosis that predominates in Latin America. It is estimated that 25 million people are under the risk of infection and, in 2008, more than 10 thousand deaths were registered. The only two drugs available in the therapeutics, nifurtimox and benznidazole, showed to be more effective in the acute phase of the disease. However, there is no standard treatment protocol effective for the chronic phase. Nitrofurazone (NF), an antimicrobial drug, has activity against T. cruzi, although being toxic. Considering the need for new antichagasic drugs, the existence of promising new therapeutic targets, as 14α-sterol demethylase and cruzain, and employing the bioisosterism and molecular hybridization approaches, four novel compounds were synthesized, characterized by melting point range, elemental analysis, IR and NMR spectroscopy. The compounds were tested against T. cruzi amastigotes in infected U2OS cells. All compounds showed selectivity towards T. cruzi and showed trypanomicidal activity in low micromolar range. The compound 3 showed potency similar to benznidazole, but lower efficacy. These results highlight the importance of the 1,2,4-triazole, thiosemicarbazonic and nitro group moieties for designing new efficient compounds, potentially for the chronic phase of Chagas disease.
Antibacterial drug and preparation method thereof
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Paragraph 0028; 0038-0040; 0058; 0059, (2020/06/20)
The invention discloses an antibacterial drug. The antibacterial drug is 2-(2,4-difluorophenyl)-1-(1H-1,2,4-triazol-1-yl)-3-(1H-1,2,3,4-tetrazol-1-yl)-2-propanol, the compound is obtained by modifyingfluconazole and introducing a tetrazole ring. Compared with fluconazole, the compound has wider antimicrobial activity spectrum. The invention also discloses a preparation method of the antibacterialdrug. The method comprises the step of introducing the tetrazole ring to obtain 2-(2,4-difluorophenyl)-1-(1H-1,2,4-triazol-1-yl)-3-(1H-1,2,3,4-tetrazol-1-yl)-2-propanol on the basis of retaining moststructures with drug effects on fluconazole.
Preparation method of 2' 4'-difluoro-2-[1-(1H-1, 2, 4-triazolyl)] acetophenone
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Paragraph 0028; 0035-0036, (2020/08/27)
The invention provides a preparation method of 2' 4'-difluoro-2-[1-(1H-1, 2, 4-triazolyl)] acetophenone. 2-chloro-2' 4'-difluoroacetophenone serving as a raw material reacts with 3-chloro-1, 2, 4-triazole to obtain 2-(3-chloro-1H-1, 2, 4-triazolyl-1-(2, 4-difluorophenyl) ethanone, and then palladium-on-carbon hydrogenation dehalogenation is carried out to obtain a final product 2' 4'-difluoro-2-[1-(1H-1, 2, 4-triazolyl) acetophenone. The method for preparing 2' 4'-difluoro-2-[1-(1H-1, 2, 4-triazolyl)] acetophenone is simple in steps, convenient to operate, low in economic cost, suitable for industrial production, capable of bringing good social benefits and economic benefits and large in economic value potential.