New derivatives of the anti-inflammatory, leprostatic drug dapsone 4 are synthesized, characterized and biologically screened by the treating the drug dapsone with chloroacetyl chloride in the presence of base. Both amino groups are acylated to give compound 6. The symmetrical acylated product then treated with Phenol, N-Acetyl-p-aminophenol, p-Chlorophenol, m-Chlorophenol, o-Hydroxybezoic acid and m-Hydroxybezoic acid to give compounds 8(a-f). The antimicrobial activity was tested for the synthesized compounds; activates were good compared to the parent drug. All the new compounds have scanned for their biological activities toward gram ‒ve and gram +ve (M. tuberculosis, S. pneumoniae, E. coli and P. mirabilis) bacteria, the synthesized derivatives gave moderate to good activity toward both mentioned types of bacteria.
New series of 4,4'-((2-(Aryl)-1H-benzo[d]imidazole1,3(2H)-diyl)bis(methylene))Diphenol(3a-g) was successfully synthesized from cyclization of the reduction product of bis Schiff bases (2) with aryl aldehydes bearing phenolic hydroxyl in the presence of acetic acid. The structure of these compounds was identified from FT-IR, 1H NMR, 13C NMR and EIMs. The Antioxidant capability was screened by DPPH and FRAP assays. Both assays showed antioxidant capability more than BHT as well. Compounds 3b and 3c showed antioxidant capacity slightly less than ascorbic acid. The docking study for theses compound was carried out as III DNA polymerase inhibitor. The results of docking demonstrated that the increase in hinderances around phenolic hy
... Show MoreThe purpose of this research work is to synthesize conjugates of some NSAIDs with sulfamethoxazole as possible mutual prodrugs to overcome the local gastric irritation of NSAID with free carboxyl group by formation of ester linkage that supposed to remain intact in stomach and may hydrolyze in intestine chemically or enzymatically; in addition to that attempting to target the synthesized derivative to the colon by formation of azo group that undergo reduction only by colonic bacterial azo reductaze enzyme to liberate the parent compound to act locally (treatment of inflammation and infections in colon)
The purpose of this research work is to synthesize conjugates of some NSAIDs with sulfamethoxazole as possible mutual prodrugs to overcome the local gastric irritation of NSAID with free carboxyl group by formation of ester linkage that supposed to remain intact in stomach and may hydrolyze in intestine chemically or enzymatically; in addition to that attempting to target the synthesized derivative to the colon by formation of azo group that undergo reduction only by colonic bacterial azo reductaze enzyme to liberate the parent compound to act locally (treatment of inflammation and infections in colon).
Key words: Mutual prodrug, Ester linkage, Azo bond, Colon targeting
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Implementations of Transition Metal complexes of shiff Base Derived Ampyrone
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Alizarin is one of the popularly used and wide separated compounds with a chemical name (1,2- dihydroxy-9,10-anthraquinone) which belong to the anthraquinones family that contain three aromatic conjugated rings and in the central rings it contains two ketonic groups.1
The coronavirus-pandemic has a major impact on women's-mental and physical-health. Polycystic-ovary-syndrome (PCOS) has a high-predisposition to many cardiometabolic-risk factors that increase susceptibility to severe complications of COVID-19 and also exhibit an increased likelihood of subfertility. The study includes the extent of the effect of COVID-19-virus on renin-levels, glutathione-s-transferase-activity and other biochemical parameters in PCOS-women. The study included 120 samples of ladies that involved: 80 PCOS-patients, and 40 healthy-ladies. Both main groups were divided into subgroups based on COVID-19 infected or not. Blood-samples were collected from PCOS-patients in Kamal-Al-Samara Hospital, at the period between Decembe
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new six mixed ligand complexes of some transition metal ions Manganese (II), Cobalt(II), Iron (II), Nickel (II) , and non transition metal ion zinc (II) And Cadmium(II) with L-valine (Val H ) as a primary ligand and Saccharin (HSac) as a secondary ligands have been prepared. All the prepared complexes have been characterized by molar conductance, magnetic susceptibility infrared, electronic spectral, Elemental microanalysis (C.H.N) and AA . The complexes with the formulas [M(Val)2(HSac)2] M= Mn (II) , Fe (II) , Co(II) ,Ni(II), Cu (II),Zn(II) and Cd(II) L- Val H= (C5H11NO2) , C7H5NO3S The study shows that these complexes have octahedral geometry; The metal complexes have been screened for their in microbiological activities against bacteria.
... Show MoreSchiff base (methyl 6-(2- (4-hydroxyphenyl) -2- (1-phenyl ethyl ideneamino) acetamido) -3, 3-dimethyl-7-oxo-4-thia-1-azabicyclo[3.2.0] heptane-2-carboxylate)Co(II), Ni(II), Cu (II), Zn (II), and Hg(II)] ions were employed to make certain complexes. Metal analysis M percent, elemental chemical analysis (C.H.N.S), and other standard physico-chemical methods were used. Magnetic susceptibility, conductometric measurements, FT-IR and UV-visible Spectra were used to identified. Theoretical treatment of the generated complexes in the gas phase was performed using the (hyperchem-8.07) program for molecular mechanics and semi-empirical computations. The (PM3) approach was used to determine the heat of formation (ΔH˚f), binding energy (ΔEb), an
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