Synthesis, physico-chemical properties and microsomal stability of compounds bearing aliphatic trifluoromethoxy group
| Autor: | Valentyna O. Pivnytska, Yevheniia Markushyna, Yuliya Tokaryeva, Günter Haufe, Oleksandr O. Grygorenko, Maria Kliachyna, Ivan G. Logvinenko, Ivan S. Kondratov, Bohdan V. Vashchenko |
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| Rok vydání: | 2020 |
| Předmět: |
Chemical substance
010405 organic chemistry Chemistry Organic Chemistry Substituent Metabolic stability 010402 general chemistry 01 natural sciences Biochemistry 0104 chemical sciences Inorganic Chemistry chemistry.chemical_compound Group (periodic table) Amide Lipophilicity Microsome Environmental Chemistry Organic chemistry Physical and Theoretical Chemistry Solubility |
| Zdroj: | Journal of Fluorine Chemistry. 231:109461 |
| ISSN: | 0022-1139 |
| DOI: | 10.1016/j.jfluchem.2020.109461 |
| Popis: | Effects of the trifluoromethoxy substituent on physico-chemical properties of compounds, such as kinetic solubility, lipophilicity and microsomal clearance, was studied in a series of aliphatic derivatives. It was found that kinetic solubility of the CF3O-containing compounds was comparable to that of analogs, i.e. compounds bearing CH3O and CF3 moieties. The CF3O-substituted compounds had higher lipophilicity as compared to methoxy analogues, and nearly the same like CF3-bearing compounds. Microsomal stability studies indicated that the trifluoromethoxy group typically decreased metabolic stability of the corresponding derivatives as compared to either CH3O- or CF3-substituted counterparts, except for N-alkoxy(sulfon)amide series. |
| Databáze: | OpenAIRE |
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