Malleshappa noolvi (18 Ergebnisse)

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Taschenbuch. Zustand: Neu. nach der Bestellung gedruckt Neuware - Printed after ordering - A new series of isoindoline-1,3-dione derivatives were synthesized by using 2-(3-bromopropyl)isoindoline-1,3-dione and phenoxy acetic acids or quinoline. The reaction was monitored by TLC using suitable mobile phase and also determined the melting point and other characterization like IR, 1H NMR, 13C NMR and Mass spectral analysis. When designing new molecules as anti-alzheimer agents, first we carried out in silico study in which isoindoline containing reference molecules as well as active site containing ligand (Donepezil) were docked using PDB 1EVE, Acetylcholinesterase enzyme, the docking study suggested interaction with PAS and CAS is essential for anti- alzheimer activity. Then we docked new molecules, they showed same interaction as that of reference molecules. Based upon docking study molecules were synthesized and screened for in vitro anti-alzheimer activity by using Ellman assay. The Compound (7a) showed good anti-Alzheimer activity with IC50 = 32nM. In docking study as well as in vitro study we found compound 7a as promising anti-alzheimer agent. Based upon the results we conclude that these molecules can act as good anti- alzheimer agents.…

Zustand: New. Dieser Artikel ist ein Print on Demand Artikel und wird nach Ihrer Bestellung fuer Sie gedruckt. Autor/Autorin: More Uttam A.Dr. Uttam A. More an Associate Professor at the Department of Pharmaceutical Chemistry in Shree Dhanvantary Pharmacy College, Kim. Dr. More and his research group focuses mainly on design and synthesis of various hetero.…

Kartoniert / Broschiert. Zustand: New. Dieser Artikel ist ein Print on Demand Artikel und wird nach Ihrer Bestellung fuer Sie gedruckt. Autor/Autorin: Karpoormath RajshekharDr. R. Karpoormath is professor at the faculty in the Dis. of Pharmaceutical Sciences, University of KwaZulu-Natal, Durban, South Africa. His research interests are: target based drug design (HIV, Cancer and TB). …

Zustand: New. Dieser Artikel ist ein Print on Demand Artikel und wird nach Ihrer Bestellung fuer Sie gedruckt. Autor/Autorin: Sidat Parin SParin S. Sidat is working as Assistant Professor in Department of Pharmaceutical chemistry at Shree Dhanvantary Pharmacy College, Kim, Surat, Gujarat. She has completed M Pharm in Pharmaceutical Chemistry from Gujarat Te.…

Zustand: New. Dieser Artikel ist ein Print on Demand Artikel und wird nach Ihrer Bestellung fuer Sie gedruckt. Autor/Autorin: Patel HarunDr. Harun M. Patel was born on 5th September 1983. He received Gold Medal in graduation and post graduation. Completed his doctoral study at Punjab Technical University-Jalndhar as Young Scientist (DST). Recently completed.…

Taschenbuch. Zustand: Neu. nach der Bestellung gedruckt Neuware - Printed after ordering - A new series of imidazo[2,1-b][1,3,4]thiadiazoles 5(a-g), 6(a-g), 9(a-i) and 12(a-h) were synthesized. Among them, 23 compounds 5a, 5b, 5e, 5d, 5f, 5g, 6a, 6b, 6c, 6d, 6e, 9b, 9d, 9f, 9g, 9h, 9i, 12b, 12c, 12d, 12e, 12g, and 12h were evaluated at National Cancer Institute for single dose in vitro primary cytotoxicity assay. Compound 5b, 5e, 6c, 6d, 6e, 12c, 12d and 12e were further screened for 5-log dose molar range as they have shown prominent cell growth inhibition at 10-5 M concentration against variety of cell lines. Compound 5e shows significant inhibition against Leukemia HL-60 cell line with GI50 of 0.0285 µM and highest selectivity towards the Leukemic Cancer cell line (selectivity ratio of 7.96) it also shows prominent ALK5 inhibition (IC50 = 0.0263 µM) and elective inhibition (91%) against KDR at10 µM. The binding mode of compound 5e by SP docking studies shows that it fits well into the active site cavity of ALK5 by forming broad and tight interactions. Lipinski's rule and in silico ADME pharmacokinetic parameters are within the acceptable range defined for human use thereby indicating their potential as a drug-like molecules. …

Zustand: New. Dieser Artikel ist ein Print on Demand Artikel und wird nach Ihrer Bestellung fuer Sie gedruckt. Autor/Autorin: Jain Payal S.Ms. Payal S. Jain PhD Scholar in Pharmaceutical Chemistry at Shree Dhanvantary College of Pharmacy, Gujarat Technological University, Ahmedabad, Gujarat. She is GPAT qualified in the year of 2014. Her Research Interest .…

Taschenbuch. Zustand: Neu. nach der Bestellung gedruckt Neuware - Printed after ordering - Eine neue Reihe von Isoindolin-1,3-Dion-Derivaten wurde unter Verwendung von 2-(3-Brompropyl)isoindolin-1,3-Dion und Phenoxyessigsäuren oder Chinolin synthetisiert. Die Reaktion wurde durch TLC mit geeigneter mobiler Phase überwacht und auch der Schmelzpunkt und andere Charakterisierungen wie IR, 1H NMR, 13C NMR und Massenspektralanalyse bestimmt. Bei der Entwicklung neuer Moleküle als Anti-Alzheimer-Wirkstoffe führten wir zunächst eine In-silico-Studie durch, bei der isoindolinhaltige Referenzmoleküle sowie ein Ligand, der das aktive Zentrum enthält (Donepezil), mit Hilfe von PDB 1EVE, dem Enzym Acetylcholinesterase, angedockt wurden. Dann haben wir neue Moleküle angedockt, die dieselbe Wechselwirkung wie die Referenzmoleküle zeigten. Auf der Grundlage der Docking-Studie wurden die Moleküle synthetisiert und mit Hilfe des Ellman-Tests auf ihre In-vitro-Aktivität gegen Alzheimer untersucht. Die Verbindung (7a) zeigte eine gute Anti-Alzheimer-Aktivität mit IC50 = 32nM. Sowohl in der Docking-Studie als auch in der In-vitro-Studie erwies sich die Verbindung 7a als vielversprechender Anti-Aalzheimer-Wirkstoff. Auf der Grundlage der Ergebnisse kommen wir zu dem Schluss, dass diese Moleküle als gute Anti-Alzheimer-Mittel wirken können.…

Taschenbuch. Zustand: Neu. nach der Bestellung gedruckt Neuware - Printed after ordering - Una nuova serie di derivati dell'isoindolina-1,3-dione è stata sintetizzata utilizzando il 2-(3-bromopropil)isoindolina-1,3-dione e acidi acetici fenossi o chinolina. La reazione è stata monitorata mediante TLC utilizzando un'adeguata fase mobile e determinando anche il punto di fusione e altre caratterizzazioni come IR, 1H NMR, 13C NMR e analisi spettrale di massa. Per la progettazione di nuove molecole come agenti anti-alzheimer, abbiamo dapprima condotto uno studio in silico in cui le molecole di riferimento contenenti isoindoline e il ligando contenente il sito attivo (Donepezil) sono stati agganciati utilizzando il PDB 1EVE, enzima acetilcolinesterasi; lo studio di docking ha suggerito che l'interazione con PAS e CAS è essenziale per l'attività anti-alzheimer. Poi abbiamo inserito nuove molecole, che hanno mostrato la stessa interazione delle molecole di riferimento. Sulla base dello studio di docking, le molecole sono state sintetizzate e sottoposte a screening per l'attività anti-alzheimer in vitro utilizzando il saggio di Ellman. Il composto (7a) ha mostrato una buona attività anti-Alzheimer con IC50 = 32nM. Nello studio di docking e in quello in vitro abbiamo trovato il composto 7a come promettente agente anti-Alzheimer. Sulla base dei risultati ottenuti, concludiamo che queste molecole possono agire come buoni agenti anti-Alzheimer.…

Taschenbuch. Zustand: Neu. nach der Bestellung gedruckt Neuware - Printed after ordering - Uma nova série de derivados de isoindolina-1,3-diona foram sintetizados utilizando ácidos 2-(3-bromopropil)isoindolina-1,3-diona e fenoxi acético ou quinolina. A reacção foi monitorizada por TLC usando fase móvel adequada e também determinou o ponto de fusão e outras caracterizações como IR, 1H NMR, 13C NMR e análise espectral de massa. Ao conceber novas moléculas como agentes anti-alzheimer, primeiro realizámos um estudo silico no qual as moléculas de referência contendo isoindolina, bem como o sítio activo contendo ligand (Donepezil) foram ancorados utilizando PDB 1EVE, enzima Acetilcolinesterase, o estudo de ancoragem sugeriu que a interacção com PAS e CAS é essencial para a actividade anti-alzheimer. Depois atracamos novas moléculas, elas mostraram a mesma interacção que as moléculas de referência. Com base no estudo de acoplamento, as moléculas foram sintetizadas e rastreadas para a actividade anti-alzheimer in vitro, utilizando o ensaio de Ellman. O Composto (7a) mostrou boa actividade anti-alzheimer com IC50 = 32nM. No estudo docking, bem como no estudo in vitro, encontramos o composto 7a como promissor agente anti-alzheimer. Com base nos resultados, concluímos que estas moléculas podem actuar como bons agentes anti-alzheimer.…