- Synthesis, characterization, andcomputational studies on phthalic anhydride-based benzylidene-hydrazide derivatives as novel,potential anti-inflammatory agents
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A series of phthalic anhydride-based substituted benzylidene-hydrazide derivatives (3a-i) was synthesized. The synthesized derivatives were authenticated by TLC, UV-visible, FTIR, NMR, and mass spectroscopic techniques and further screened for in vivo anti-inflammatory and analgesic activities by carrageenan-induced rat paw oedema and tail immersion methods, respectively, using diclofenac sodium as standard drug. The derivatives 3d, 3e, and 3h were found to be most active anti-inflammatory and analgesic agents among all the synthesized derivatives. The physico-chemical similarity of the derivatives with standard drugs was assessed by calculating various physicochemical properties using software programs. The percent similarity of synthesized derivatives was found to be good except 3i. The derivatives were subjected to QSAR by multilinear regression using Analyze it version 3.0 software and two statistically sound models were developed with R2 (0.933-0.960), Radj2 (0.595-0.762) and Q2 (0.999) with good F (2.76-4.84) values. Molecular docking studies were performed by MVD software (version 2012.5.0.0). The derivative 3h has emerged out as most potent anti-inflammatory agent with highest dock score, i.e., -93.64. Springer Science+Business Media 2013.
- Kajal, Anu,Bala, Suman,Kamboj, Sunil,Saini, Vipin
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p. 2676 - 2689
(2014/05/06)
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- Design and synthesis of 2-(1, 3-dioxoisoindolin-2-yl)-N-(4-oxo-2- substitutedthiazolidin-3-yl) acetamide derivatives as potential anticonvulsant agents
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A series of 2-(1,3-dioxoisoindolin-2-yl)-N-(4-oxo-2-substitutedthiazolidin- 3-yl) acetamide derivatives were designed and synthesized using appropriate synthetic route, keeping in view the structural requirement of pharmacophore and evaluated for anticonvulsant activity and CNS depressant activities in mice. The synthesized derivatives were examined in the maximal electroshock seizure (MES), subcutaneous pentylenetetrazole (sc-PTZ) induced seizure and neurotoxicity screens and were also evaluated for behavioral activity. All the tested compounds showed protection against MES test indicative of their ability to inhibit the seizure spread.
- Nikalje, Anna Pratima G.,Khan, Firoz Kalam,Ghodke, Mangesh
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experimental part
p. 5448 - 5455
(2011/12/14)
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