A simple, versatile, one-pot, multi-component reaction (MCR) of ethyl 6-amino-5-cyano-2-methyl-4H-pyran-3-carboxylate derivatives has been achieved in the presence of urea as a potent catalyst in water-ethanol as a green solvent system. Reaction was proceeding via three component reaction by utilizing various aldehyde, malononitrile and ethylacetoacetate at room temperature. All Synthesized products were confirmed by Mass, 1H-NMR, IR and Melting point. Mild reaction conditions, excellent yields, easy isolation of products, no column chromatographic separation, reusability of reaction media.
A simple, versatile, one-pot, multi-component reaction (MCR) of ethyl 6-amino-5-cyano-2-methyl-4H-pyran-3-carboxylate derivatives has been achieved in...
This book describes series of quinoline hybrid thiosemicarbazide derivatives under microwave irradiation. Synthesized compounds were successfully applied against the biological studies. The docking study suggested that selected molecules were perfect, fit into the protein cavity with excellent G-score. Molecular dynamics study with protein (PDB: 3JSU) studied in Schrodinger software, Pharmacophore study and ADME-Tox were carried out for the drug-likeness properties. This study proved that our molecules could act as hit molecules in the future.
This book describes series of quinoline hybrid thiosemicarbazide derivatives under microwave irradiation. Synthesized compounds were successfully appl...
Patel, Dhaval B., Patel, Siddharth S., Patel, Hitesh D.
Novel fluorine containing quinoline hybrid thiosemicarbazide analogues and screened for their in-vitrostudy in antibacterial, antifungal, antimalarial, antituberculosis strains. Analogues were active against antimalarial Plasmodium falciparum strain, among them analogues 8d, 8g, 8h, 8k and 8l shown remarkable activity than reference drug Quinine. We have carried out Molecular docking, ADME-Tox, Molecular dynamics and Pharmacophore study. Biological activity and Molecular docking study were correlated for the potent molecules. This study were suggested active binding site of analogues to give...
Novel fluorine containing quinoline hybrid thiosemicarbazide analogues and screened for their in-vitrostudy in antibacterial, antifungal, antimalarial...
In this book, we have a described novel series of fluorine containing quinoline hybrid thiosemicarbazide analogues (8a-8l) by modern medicinal chemistry and have led to large number of effective drugs. We have synthesized novel fluorine containing quinoline hybrid thiosemicarbazide analogues and tested for their in-vitro study in antibacterial, antifungal, antimalarial, antituberculosis strains. With this study, we concluded that N- based heterocyclic compounds having potency for biological activity.
In this book, we have a described novel series of fluorine containing quinoline hybrid thiosemicarbazide analogues (8a-8l) by modern medicinal chemist...
In this book we have established a novel series of 2-(2-chlorophenyl)quinoline-4-carboxylic acid based thiosemicarbazide derivatives all compounds are conforming by their physical data (melting point) and spectral data (Mass analysis , 1H NMR, 13C NMR). All compounds are analyzing in antibacterial and antifungal Biological activity. In biological analysis we have found that many compounds have potent activity against different strains.
In this book we have established a novel series of 2-(2-chlorophenyl)quinoline-4-carboxylic acid based thiosemicarbazide derivatives all compounds are...
In this book, we have established a green and highly efficient one-pot three component microwave irradiation protocol for the synthesis of various quinoline-4-carboxylic acidscatalyzed by p-TSA. The p-TSA catalyst was easily commercially available and non-hazardous. There are many features of this protocol including high yield of products with high purity as well as lower reaction time compared to conventional methods, a simple work-up processand avoidance of the use of hazardous organic solvents.A simple work-up procedure make the present method a valuable contribution in agreement with...
In this book, we have established a green and highly efficient one-pot three component microwave irradiation protocol for the synthesis of various qui...
In this book, we have discussed and to per best of our knowledge, we are the foremost in reporting water and ethanol as a solvent in the synthesis of ethyl 6-amino-5-cyano-2-methyl-4H-pyran-3-carboxylate derivative using Urea as a novel catalyst under the short period of time. This clearly shows that all substrates react smoothly under optimal conditions to give direct products with high yields. Subsequently, we demonstrated that benzaldehyde and the aromatic aldehydes bearing electron-withdrawing groups (such as nitro or halogens) require a shorter reaction time and give better yields than...
In this book, we have discussed and to per best of our knowledge, we are the foremost in reporting water and ethanol as a solvent in the synthesis of ...
In summary, this work demonstrates the designing, synthesis and biological evaluation of novel 2-(2-chlorophenyl)quinoline-4-carboxylic acid hybrid thiosemicarbazides. The synthesized derivatives were evaluated for their variousin-vitro biological activities. Most of the compounds displayed excellent activity against gram-positive bacteria in comparison to gram-negative bacteria. Biological activity and docking results of quinoline derivatives makes interesting lead in drug development. The calculated ADME-Tox parameters suggest good pharmacokinetic properties. These studies disclose that...
In summary, this work demonstrates the designing, synthesis and biological evaluation of novel 2-(2-chlorophenyl)quinoline-4-carboxylic acid hybrid th...
In summary Series of new 2-(2-chlorophenyl)quinoline-4-carboxylic acid-based thiosemicarbazide were synthesized in excellent yields. Synthesized derivatives were characterized by spectral studies 1H NMR, 13C NMR, mass spectrometry, IR analysis, elemental analyses and physical studies of Melting points. All the newly synthesized compounds were screened for biological activity and the results showed good activity compared to the standard drug.
In summary Series of new 2-(2-chlorophenyl)quinoline-4-carboxylic acid-based thiosemicarbazide were synthesized in excellent yields. Synthesized deriv...