- Ruthenium Catalyzed N-Alkylation of Cyclic Amines with Primary Alcohols
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A robust alcohol amination protocol using common saturated amines and primary alcohols as starting materials is described. The reactions are catalyzed by combination of dichloro(p-cymene)ruthenium(II) dimer precatalyst with triphenylphosphine ligand, with
- Savela, Risto,Vogt, Dieter,Leino, Reko
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p. 3030 - 3040
(2020/05/22)
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- Alkylated Piperazines and Piperazine-Azole Hybrids as Antifungal Agents
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The extensive use of fluconazole (FLC) and other azole drugs has caused the emergence and rise of azole-resistant fungi. The fungistatic nature of FLC in combination with toxicity concerns have resulted in an increased demand for new azole antifungal agents. Herein, we report the synthesis and antifungal activity of novel alkylated piperazines and alkylated piperazine-azole hybrids, their time-kill studies, their hemolytic activity against murine erythrocytes, as well as their cytotoxicity against mammalian cells. Many of these molecules exhibited broad-spectrum activity against all tested fungal strains, with excellent minimum inhibitory concentration (MIC) values against non-albicans Candida and Aspergillus strains. The most promising compounds were found to be less hemolytic than the FDA-approved antifungal agent voriconazole (VOR). Finally, we demonstrate that the synthetic alkylated piperazine-azole hybrids do not function by fungal membrane disruption, but instead by disruption of the ergosterol biosynthetic pathway via inhibition of the 14α-demethylase enzyme present in fungal cells.
- Thamban Chandrika, Nishad,Shrestha, Sanjib K.,Ngo, Huy X.,Tsodikov, Oleg V.,Howard, Kaitlind C.,Garneau-Tsodikova, Sylvie
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p. 158 - 173
(2018/02/10)
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- N - alkylpiperazine purification of
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PROBLEM TO BE SOLVED: To provide a purification method of N-alkyl piperazines, capable of providing high purity N-alkyl piperazines with low cost and having a high recovery rate.SOLUTION: A mixture of N-alkyl piperazines and a piperazine is distilled in the presence of a polar organic solvent having a higher boiling point than that of the piperazine.
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Paragraph 0053
(2017/02/28)
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- CARBODITHIOATES WITH SPERMICIDAL ACTIVITY AND PROCESS FOR PREPARATION THEREOF
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The present invention relates to the synthesis and biological evaluation of compound of formula I as spermicidal agents, and its pharmaceutically acceptable acid salt thereof. The invention provides bis(4- substituted-1-piperazinylthiocarbonyl) disulfide (when n = 0) and alkane-1,n-diylbis(4-substituted piperazine-1-carbodithioate) (when n = 0, 1, 2 or 3) as shown in figure 1 of the accompanying drawing. These compounds are found to be useful for spermicidal activity.
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Page/Page column 34
(2014/08/20)
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- Ultrasound effect on the synthesis of 4-alkyl-(aryl)aminobenzaldehydes
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The sonochemical nucleophilic aromatic substitutions on 4-fluorobenzaldehyde with different azacycloalkanes and azoles have been studied. A beneficial ultrasound effect was observed, reactions were clean and high yields of the products were isolated after 15 min sonication.
- Magdolen, Peter,Me?iarová, Mária,Toma, ?tefan
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p. 4781 - 4785
(2007/10/03)
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