A series of Schiff base-bearing salicylaldehyde moiety compounds (1-4) had been designed, synthesized, subjected to insilico ADMET prediction, molecular docking, characterization by FT-IR, and CHNS analysis techniques, and finally to their Anti-inflammatory profile using cyclooxygenase fluorescence inhibitor screening assay methods along with standard drugs, celecoxib, and diclofenac. The ADMET studies were used to predict which compounds would be suitable for oral administration, as well as absorption sites, bioavailability, TPSA, and drug likeness. According to the results of ADME data, all of the produced chemicals can be absorbed through the GIT and have passed Lipinski’s rule of five. Through molecular docking with PyRx 0.8, these synthesized compounds were tested insilico selectivity toward COX-1 and COX-2 and in vitro for their anti-inflammatory efficacy . In vitro testing demonstrated that all of the produced compounds had significantly stronger activity against the COX-2 enzyme than COX-1. Among these, compound 1 displayed the most potent inhibitory activity with an IC50 value of 0.19 µM compared to standard drug celecoxib (IC50 = 0.29 µM). The most active derivative compound1 was oriented towards the active site and occupied the target enzyme based on the docking investigation against COX-1 and COX-2. In addition, insilico investigations found that COX-2 has a higher inhibitory activity than COX-1
Objective:This study involved synthesis of a new series of different five-membered heterocyclic derivatives, testing their antioxidant activity, and examining their potential in vitro antimicrobial agents. Methods: The synthesis of the derivatives involved a three-step process. Initially, succinyl chloride was reacted with methanol, followed by a reaction with 80% hydrazine hydrate through a nucleophilic addition-elimination mechanism, resulting in the formation of succinohydrazide (I). This compound was then employed as a precursor for the synthesis of Schiff bases (II), and (III) by reacting it with m-nitro benzaldehyde and p-nitro benzaldehyde. Following this, a ring closure reaction was applied using thioglycolic acid, glycolic acid,
... Show MoreGreen synthesis is depending on preparation of nano composited SiO2/V2O5 by using the modified sol-gel method depending on rice husk ash as a source for the extraction of silica gel and the product powder of nano composited SiO2/V2O5 characterization by many techniques such as X-ray diffraction spectroscopy (XRD), field emission scanning electron microscopy (FESEM), and N2 adsorptions/desorption isotherms (BET). This study also includs the biological effectiveness of SiO2/V2O5 and its effect on inhibiting bacterial growth after the prepared nanomaterial was applied to wound dressings, which gave a promising result for its use as
... Show MoreNew Fourteen compounds were synthesized in four steps. The first step included synthesis of 2-biphenyl fused ring of imidazo(1,2- a)pyrimidine from the reaction of 2-aminopyrimidine and biphenyl phenacyl bromide . The second step was introduced aldehyde group from the reaction of 2-biphenyl fused rings of imidazo(1,2-a)pyrimidine with POCl3 in presence of DMF and CHCl3. 3-Carbaladehyde derivatives of fused imidazo/pyrimidine was reacted with different aromatic amines to afford new Schiff bases. These new 3- imines derivatives was reduced by using sodiumborohydride to yield another new 3-aminomethyl-2-biphenyl imidazo (1,2-a)pyrimidine derivatives in moderate yield .Some new prepared compounds were identified by melting point, FT- IR , 13C-
... Show MoreThis paper deals with the ideological positioning of the English poet John Donne in a selected poems of his i.e Holy Sonnet X, as regards the theme of death found therein. The researchers adopt an emerging branch of stylistics, called Critical Stylistics, as proposed by Jeffries (2010) in order to uncover the ideologies of the author regarding the topic concerned and how linguistic choices are used to slant ideas. The model is comprised of ten tools of analysis which, upon being applied to the selected data, have shown how the poet exploits language resources in order to pass his ideology and influence his readers. In this paper, the workings of only one tool are presented as applied to a certain portion of the data.
The presence of alkaloids in Crassula ovata is a topic that is still unexplored, as there are no published studies on the matter. This study demonstrates the presence of an alkaloid compound (and its class) for the first time in Crassula ovata. The plant material was defatted with n-hexane, and a Soxhlet apparatus was used for the extraction process, while the acid-base method was used for the isolation of alkaloids from the chloroform fractions. The quaternary alkaloid was precipitated from the aqueous layer spontaneously, in high quantity. By using standard spectroscopic methods (including liquid chromatography - mass spectroscopy) we were able to clarify the structure of the precipi¬tated compound as a tetrahydroprotoberberine a
... Show More5-(mercapto-1,3,4-thiadiazole-2yl)α,α-(diphenyl)methanol have been synthesized by ring closer of potassium xanthate[which have been prepared by reaction of benzilic acid hydrazide with carbon disulphide in potassium hydroxide] using conc.sulphuric acid at (0-5)°C scheme(I). Their characterization was carried out from T.L.C, M.P, FT.IR and 1H-NMR.
In the present work, several new cyclic imides (succinimides) linked to benzothiazole or thiazole moieties through phenyl azo group were synthesized. Synthesis of the new imides was performed via multistep synthesis. The first step involved reaction of equimolar amounts of succinic anhydride and p-toluidine producing N-(4-tolyl) succinamic acid (1) which was dehydrated in the second step via treatment with acetic anhydride and anhydrous sodium acetate affording N-(4-tolyl)succinimide (2).
In the third step, substituted-2-aminobenzothiazoles were introduced in diazotization reaction with nitrous acid producing the corresponding diazonium salts and these inturn were introduced directly in coupling reaction with compound (2) affording th
In this paper, the definition of fuzzy anti-inner product in a linear space is introduced. Some results of fuzzy anti-inner product spaces are given, such as the relation between fuzzy inner product space and fuzzy anti-inner product. The notion of minimizing vector is introduced in fuzzy anti-inner product settings.
In this rescrch,new mixed ligand Schiff base complexes of Mn(II),Co(II),Ni(II),Cu(II), Cd(II), and Hg(II) are formulated from the Schiff base( L)resulting from o-phathalaldehyde(o-PA) with p-nitroaniline(p-NA)as a primary ligand and anthranilic acid as a subordinate ligand. Diagnosis of prepared Ligand and its complexes is done by spectral methods mass spectrometer;1H -NMR for ligand Schiff base FTIR, UV-Vis, molar conductance, elemental microanalyses, atomic absoption and magnetic susceptibility. The analytical studies for the all new complexes have shown octahedral geometries. The study of organicperformance of ligand Schiff base and its complexes show various activity agansit four type of bactria two gram (+) and two gram (-) .
A new class of thiadiazole /silica nanocomposites with chemical bonds between thiadiazole monomers and modified nanosilica surface were synthesized by free radical polymerization. Presence silica nanoparticles in the structure of nanocomposite showed effectively improve the physical and chemical properties of Producing polymers. A nanocomposite material with feature properties comparison with their polymers, The structure and morphology of the synthesis materials were investigated by FT-IR spectrum which display preparation new thiadiazole compounds and polymerization monomers. FT-IR showed disappeared double bond (C=C) of monomers, due to produce long chains of thiadiazole polymers and nanocomposite. X-ray diffraction gave idea ab
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