Dhaval B Patel

Dans ce livre, nous avons d crit une nouvelle s rie d'analogues de thiosemicarbazide hybrides contenant de la quinol ine et du fluor (8a-8l) par le biais de la chimie m dicinale moderne, ce qui a permis de mettre au point un grand nombre de m dicaments efficaces. Nous avons synth tis de nouveaux analogues hybrides de thios micarbazide contenant du fluor et de la quinol ine et les avons test s in vitro sur des souches antibact riennes, antifongiques, antipaludiques et antituberculeuses. Cette tude nous a permis de conclure que les compos s h t rocycliques base de N ont une activit biologique puissante.

Neste livro, temos uma nova s rie descrita de fl or contendo an logos de tiosemicarbazida h bridos de quinole na (8a-8l) pela qu mica medicinal moderna e que conduziu a um grande n mero de f rmacos eficazes. Com este estudo, conclu mos que os compostos heteroc clicos base de N- com pot ncia para a actividade biol gica.

In questo libro abbiamo stabilito una nuova serie di derivati ​​tiosemicarbazidici a base di acido 2-(2-clorofenil)chinolina-4-carbossilico tutti i composti sono conformi per i loro dati fisici (punto di fusione) e dati spettrali (analisi di massa, 1H NMR, 13C NMR ). Tutti i composti stanno analizzando l'attivit biologica antibatterica e antimicotica. Nell'analisi biologica abbiamo scoperto che molti composti hanno una potente attivit contro diversi ceppi.

Neste livro, estabelecemos uma nova s rie de derivados de tiossemicarbazida base de cido 2-(2-clorofenil)quinolina-4-carbox lico, todos os compostos s o conformes por seus dados f sicos (ponto de fus o) e dados espectrais (an lise de massa, 1H NMR, 13C NMR ). Todos os compostos est o analisando em atividade biol gica antibacteriana e antif ngica. Na an lise biol gica, descobrimos que muitos compostos t m atividade potente contra diferentes cepas.

Dans ce livre, nous avons tabli une nouvelle s rie de d riv s de thiosemicarbazide base d'acide 2-(2-chloroph nyl)quinol ine-4-carboxylique tous les compos s sont conformes par leurs donn es physiques (point de fusion) et leurs donn es spectrales (analyse de masse, RMN 1H, RMN 13C ). Tous les compos s analysent l'activit biologique antibact rienne et antifongique. Dans l'analyse biologique, nous avons d couvert que de nombreux compos s ont une activit puissante contre diff rentes souches.

In diesem Buch haben wir eine neue Serie von 2-(2-Chlorphenyl)chinolin-4-carbons ure-basierten Thiosemicarbazid-Derivaten etabliert, wobei alle Verbindungen durch ihre physikalischen Daten (Schmelzpunkt) und spektralen Daten (Massenanalyse, 1H-NMR, 13C-NMR) bereinstimmen ). Alle Verbindungen werden auf antibakterielle und antimykotische biologische Aktivit t analysiert. Bei der biologischen Analyse haben wir festgestellt, dass viele Verbindungen eine starke Aktivit t gegen verschiedene St mme aufweisen.

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.

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.

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.

In this book author has described a series of new 2-(2-chlorophenyl)quinoline-4-carboxylic acid based thiosemicarbazide were synthesized in extremely good yields. Synthesized derivatives were characterized by spectral studies 1H NMR, 13C NMR, mass spectrometry, IR analysis, elemental analyses and physical studies 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, 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 active molecules are used as term plate for the development of active biological agents. Molecular dynamics simulation can be concluded that MD can be successfully implemented for new drug development and several promising inhibitor molecules.

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.

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 a best mechanism in in-silico side. Then, most active molecule 8g was performed for the molecular dynamics study. Here, this article concluded that analogues 8d, 8g and 8k were representing a promising lead for the new development of antimalarial therapeutics.

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.

We have synthesized a series of quinoline hybrid thiosemicarbazide derivatives under microwave irradiation. Synthesized compounds were successfully applied against the biological studies. Compounds 7a, 7g, 7k exhibited potent activity againstP. aeruginosa, compounds 7a, 7f,7h,7r showed excellent activity against E.coli, compounds 7a, 7b, 7c, 7e, 7f, 7l, 7o, 7p, 7q and 7sexhibited good activity against plasmodium falciparum strain. The docking study was performed on selected three proteins 3JSU, 4DP3 and 1J3K. Compounds7b (-8.32) and 7i (-8.22) were selected in 3JSU, compounds7c (-7.23) and 7l (-5.82) were selected in 4DP3 for the best binding possess, compounds7b (-4.323) and 7l (-3.039) were selected in 1J3Kfor the best binding possess. The docking study was suggested that selected molecules were perfect, fit into the protein cavity with excellent G-score. Molecular dynamics study of compound 7ewith 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 be act as hit molecules in the future.