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
The dictionary meaning of the word is a linguistic category of the thing in a specific way . it is also a brief description of it .The main function of the concept lies in the total scientific reflection of the things where as the main function of the meaning is a brief reference to a certain content (extralinguistic ) which shows human knowledge . The meaning is (a storage unit ) of knowledge of the world ,but this does not give the extra linguistic meaning which the old words have . Hence, additional cultural ,ethnic,communicative
and genetic information is needed.
All the old words which are brought into us
... Show MoreThe corrosion protection of low carbon steel in 2.5 M HCl solution by kiwi juice was studied at different temperatures and immersion times by weight loss technique. To study the determination of the optimum conditions from statistical design in evaluation of a corrosion inhibitor, three variables, were considered as the most dominant variables. These variables are: temperature, inhibitor concentration (extracted kiwi juice) and immersion time at static conditions.
These three variables are manipulated through the experimental work using central composite rotatable Box – Wilson Experimental Design (BWED) where second order polynomial model was proposed to correlate the studied variables with the corrosion rate o
... Show MoreSeveral new derivatives of 1, 2, 4-triazoles linked to phthalimide moiety were synthesized through following multisteps. The first step involved preparation of 2, 2-diphthalimidyl ethanoic acid [2] via reaction of two moles of phthalimide with dichloroacetic acid. Treatment of the resulted imide with ethanol in the second step afforded 2, 2-diphthalimidyl ester [3] which inturn was introduced in reaction with hydrazine hydrate in the third step, producing the corresponding hydrazide derivative [4]. The synthesized hydazide was introduced in different synthetic paths including treatment with carbon disulfide in alkaline solution then with hydrazine hydrate to afford the new 1, 2, 4-triazole [10]. Reaction of compound [10] with different alde
... Show MoreBacteriocin is an important antimicrobial peptide that can be used in industrial and medical fields due to its characteristics of antibacterial, food preservation and anticancer activities. Fifty isolates of Bacillus sp were collected from different soil samples which were already recognized via morphological and biochemical identification process. The isolates were screened for bacteriocin production effective against Staphylococcus spp in order to select the highest producing isolate. The isolate NK16 showed the maximum bacteriocin production (80 AU/ml) which was further characterized as Bacillus subtilis NK 16 through using API identification system (API 20E and API 50CHB). Then, next step was to detect the optimal conditions for maximum
... Show MoreSince cancer is becoming a leading cause of death worldwide, efforts should be concentrated on understanding its underlying biological alterations that would be utilized in disease management, especially prevention strategies. Within this context, multiple bodies of evidence have highlighted leptin’s practical and promising role, a peptide hormone extracted from adipose and fatty tissues with other adipokines, in promoting the proliferation, migration, and metastatic invasion of breast carcinoma cells. Excessive blood leptin levels and hyperleptinemia increase body fat content and stimulate appetite. Also, high leptin level is believed to be associated with several conditions, including overeating, emotional stress, inflammation, obesity,
... Show MoreSynthetic anti-TB drugs are being used to treat tuberculosis (TB) as they are effective, however, they are accompanied by many side effects. The disease has remained largely uncured till date. The use of plant extracts or phytochemicals along with the anti-TB drugs is a very attractive strategy to make the treatment more effective as phytochemicals have no side-effects, are much less toxic than synthetic anti-TB drugs, are safe to use and most importantly, do not produce resistant strains as opposed to synthetic anti-TB drugs. Approximately 420,000 plant species have been identified globally and among them only a few have been explored for their therapeutic potential. Traditional medicine in different parts of the world has employed crud
... Show MoreIn this research, a Co-polymer (Styrene / Allyl-2.3.4.6-tetra-O-acetyl-β-D-glucopyranoside) was synthesized from glucose in four steps using Addition Polymerization according to the radical mechanism using Benzoyl Peroxide (BP) as initiator. Initially, Allyl-2.3.4.6-tetra-O-acetyl-β-D-glucopyranoside monomer was prepared in three steps and the reaction was followed by (HPLC, FT-IR, TLC), in the fourth step the monomer was polymerized with Styrene and the structure was determined by FT-IR and NMR spectroscopy. The reaction conditions (temperature, reaction time, material ratios) were also studied to obtain the highest yield, the relative, specific and reduced viscosity of the prepared polymer was determined, from which the viscosity ave
... Show MoreAbstract: The M(II) complexes [M2(phen)2(L)(H2O)2Cl2] in (2:1:2 (M:L:phen) molar ratio, (where M(II) =Mn(II), Co(II), Cu(II), Ni(II) and Hg(II), phen = 1,10-phenanthroline; L = 2,2'-(1Z,1'Z)-(biphenyl-4,4'-diylbis(azan-1-yl-1-ylidene))bis(methan-1-yl-1- ylidene)diphenol] were synthesized. The mixed complexes have been prepared and characterized using 1H and13C NMR, UV/Visible, FTIR spectra methods and elemental microanalysis, as well as magnetic susceptibility and conductivity measurements. The metal complexes were tested in vitro against three types of pathogenic bacteria microorganisms: Staphylococcus aurous, Escherichia coli, Bacillussubtilis and Pseudomonasaeroginosa to assess their antimicrobial properties. From this study shows that a
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