β-Keto esters from ketones and ethyl chloroformate: a rapid, general, efficient synthesis of pyrazolones and their antimicrobial, in silico and in vitro cytotoxicity studies.
Ramasamy Venkat Ragavan,K. M. Kumar,Vijayaparthasarathi Vijayakumar,S. Sarveswari,Sudha Ramaiah,Anand Anbarasu,S. Karthikeyan,Periyasamy Giridharan,Nalilu Suchetha Kumari +8 more
- Vol. 3, Iss: 1, pp 6-6
Reads0
Chats0
TLDR
A simple method to synthesize β-keto esters from ketones and ethyl chloroformate by changing the base and reagent is developed that can be useful for the synthesis of pharmaceutically important pyrazolones also.Abstract:
Background
Pyrazolones are traditionally synthesized by the reaction of β-keto esters with hydrazine and its derivatives. There are methods to synthesize β-keto esters from esters and aldehydes, but these methods have main limitation in varying the substituents. Often, there are a number of methods such as acylation of enolates in which a chelating effect has been employed to lock the enolate anion using lithium and magnesium salts; however, these methods suffer from inconsistent yields in the case of aliphatic acylation. There are methods to synthesize β-keto esters from ketones like caboxylation of ketone enolates using carbon dioxide and carbon monoxide sources in the presence of palladium or transition metal catalysts. Currently, the most general and simple method to synthesize β-keto ester is the reaction of dimethyl or ethyl carbonate with ketone in the presence of strong bases which also requires long reaction time, use of excessive amount of reagent and inconsistent yield. These factors lead us to develop a simple method to synthesize β-keto esters by changing the base and reagent.read more
Citations
More filters
Journal ArticleDOI
Core–shell structured magnetic silica supported propylamine/molybdate complexes: an efficient and magnetically recoverable nanocatalyst
TL;DR: In this paper, a core-shell structured magnetic silica supported propylamine/molybdate complex (Fe3O4@SiO2/Pr-NMo[Mo5O18]) is prepared, characterized and applied as an effective and easily recoverable nanocatalyst.
Journal ArticleDOI
Synthesis, DNA binding and in-vitro cytotoxicity studies on novel bis-pyrazoles
K. Indrasena Reddy,C. Aruna,M. Manisha,K. Srihari,K. Sudhakar Babu,Vijayaparthasarathi Vijayakumar,S. Sarveswari,R. Priya,Anantharaman Amrita,Ramamoorthy Siva +9 more
TL;DR: A new series of bis-pyrazoles 6a-t were synthesized from 3,5-dimethyl pyrazole using sequential approach and subjected to the in-vitro cytotoxicity studies against human pancreatic adenocarcinoma, human non-small cell lung carcinoma cell lines.
Journal ArticleDOI
Sedative and antinociceptive activities of two new sesquiterpenes isolated from Ricinus communis.
Umar Farooq,Ajmal Khan,Ajmal Khan,Sadia Naz,Abdur Rauf,Haroon Khan,Afsar Khan,Irfan Ullah,Syed Majid Bukhari +8 more
TL;DR: Two new sesquiterpenes, trivially named ricinusoid A and ricinusoids B, were isolated from ethyl acetate fraction of Ricinus communis and possessed marked sedative and antinociceptive effects in animal models.
Journal ArticleDOI
Potent activity of bioconjugated peptide and selenium nanoparticles against colorectal adenocarcinoma cells
TL;DR: Novel peptide-SeNPs conjugates tested in this study has a significant anticancer activity that can be potentially used for targeting the cancer cells.
References
More filters
Journal ArticleDOI
UCSF Chimera--a visualization system for exploratory research and analysis.
Eric F. Pettersen,Thomas D. Goddard,Conrad C. Huang,Gregory S. Couch,Daniel M. Greenblatt,Elaine C. Meng,Thomas E. Ferrin +6 more
TL;DR: Two unusual extensions are presented: Multiscale, which adds the ability to visualize large‐scale molecular assemblies such as viral coats, and Collaboratory, which allows researchers to share a Chimera session interactively despite being at separate locales.
Journal ArticleDOI
The Protein Data Bank
Helen M. Berman,John D. Westbrook,Zukang Feng,Gary L. Gilliland,Talapady N. Bhat,Helge Weissig,Ilya N. Shindyalov,Philip E. Bourne +7 more
TL;DR: The goals of the PDB are described, the systems in place for data deposition and access, how to obtain further information and plans for the future development of the resource are described.
Journal ArticleDOI
SWISS-MODEL and the Swiss-PdbViewer: an environment for comparative protein modeling.
Nicolas Guex,Manuel C. Peitsch +1 more
TL;DR: An environment for comparative protein modeling is developed that consists of SWISS‐MODEL, a server for automated comparativeprotein modeling and of the SWiss‐PdbViewer, a sequence to structure workbench that provides a large selection of structure analysis and display tools.
Journal ArticleDOI
Ligand docking and binding site analysis with PyMOL and Autodock/Vina.
Daniel Seeliger,Bert L. de Groot +1 more
TL;DR: An interface between the popular molecular graphics system PyMOL and the molecular docking suites Autodock and Vina is presented and it is demonstrated how the combination of docking and visualization can aid structure-based drug design efforts.
Journal ArticleDOI
GEMDOCK: A generic evolutionary method for molecular docking
Jinn-Moon Yang,Chun Chen Chen +1 more
TL;DR: GEMDOCK is a useful tool for molecular recognition and may be used to systematically evaluate and thus improve scoring functions, and found that if the scoring function was perfect, then the predicted accuracy was also essentially perfect.
Related Papers (5)
Synthesis of (E)-1-Propenyl Ketones from Carboxylic Esters and Carboxamides by Use of Mixed Organolithium-Magnesium Reagents. Synthesis of α-Damascone, β-Damascone, and β-Damascenone†
Charles Fehr,Jose Galindo +1 more