- Synthesis, antibacterial activity, and docking studies of some novel N′-benzylidene-2-(2,4,5-trifluorophenyl)acetohydrazides
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An improved method was developed for synthesis of 2,4,5-trifluorobenzohydrazide derivatives through condensation of trifluorophenylacetohydrazide with different aryl aldehydes in ethanol with 70% perchloric acid as catalyst. The developed method is efficient in terms of shorter reaction time, easy workup, and purity of final products. We synthesized a total of 25 molecules and screened them for antibacterial activity. Among the synthesized compounds, 4q showed good antibacterial activity against Streptococcus mutans MTCC 497 and Staphylococcus aureus MTCC 737 [50% inhibition concentration (IC50): 30 and 35?μg/mL, respectively], followed by compound 4c (IC50: 45?μg/mL) against Streptococcus mutans MTCC 497 as well as Salmonella enterica MTCC 3858. Molecular docking study employing glucosamine 6-phosphate deaminase (NagB) enzyme (PDB: 2RI1) revealed that the Glide scores of the present ligands played a role. Compounds with 2-NO2, 4-(NCH3)2, and 3,4-di-OH functional groups on the benzylidene ring (4e, i, m) exhibited significant Glide score of ?8.2?kcal/mol.
- Ramesh, Navudu,Gangadhara Rao, Mannem,Vasu Babu,Nagababu,Umamaheswara Rao,Hari Babu
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- Preparation method of 2, 4, 5-trifluorophenylacetic acid
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The invention provides a preparation method of 2, 4, 5-trifluorophenylacetic acid. The method comprises the following steps: 1) reacting 2, 4, 5-trifluorobromobenzene with metal magnesium to obtain 2, 4, 5-trifluorophenyl magnesium bromide; 2) reacting 2, 4, 5-trifluorophenyl magnesium bromide with halogenated acetate to prepare an intermediate A; 3) hydrolyzing the intermediate A in an alkaline solution or an acidic solution to obtain 2, 4, 5-trifluorophenylacetic acid. The structure of the intermediate A is shown as the following structure, wherein R represents a C1-C10 alkyl group. The preparation method of 2, 4, 5-trifluorophenylacetic acid provided by the invention has the advantages of simple process flow, low cost, environmental friendliness and mild conditions.
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Paragraph 0049-0064; 0071-0076
(2021/07/28)
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- NEW PROCESS FOR THE PREPARATION OF 2,4,5- TRIFLUOROPHENYLACETIC ACID"
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The present invention relates to a new process for the preparation of 2,4,5-trifluorophenylacetic acid and salts thereof by means of new synthetic intermediates.
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Paragraph 0054; 0055; 0056
(2014/03/24)
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- Process for the synthesis of trifluorophenylacetic acids
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The present invention addresses a process for the preparation of 2,4,5-trifluorophenylacetic acid using a Cu(I) salt as a catalyst.
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