During this paper, new Schiff's base derivatives [F1-F5] were prepared through the reaction of dapsone drug with different substituted benzaldehyde compounds. Schiff's bases were then converted into 2,3-dihyroquinazolin-4(1H)-one derivatives [F6-F10] through the reaction with 2-amino benzoic acid in ethanol. The synthesized compounds were identified by their physical properties using UV-Vis, FT-IR and 1H-NMR analyses. The liquid crystalline properties of some prepared compounds revealed smectic and nematic phases. Using two separate bacterial species, Pseudomonas aeruginosa (Gram -ve) and Staphylococcus aureus (Gram +ve), the antimicrobial activities of certain synthesized compounds [F1,F2,F7,F8] were investigated using the agar diffusion process. The findings revealed that some of the assayed compounds had antimicrobial activities against the bacteria tested.
The new C-5 schiff bases derived from D-erythroascorbic acid contaning pyrimidine unit were synthesized by condensation of D-erythroascorbic acid with aromatic amine (containing pyrimidine unit)in dry benzene using glacial acetic acid as a catalyst. D-erythroascorbic acid was synthesized by four steps(Schem 1), while the aromatic amine which is containing oxopyrimidine or thiopyrimidine synthesized by the reaction of chalcone urea or thiourea in acid or basic medium, respectively . The structure of synthesized compounds have been characterized by their melting
... Show MoreThe research includes the synthesis and identification of the mixed ligands complexes of M 2 Ions in general composition ,[M(Leu) 2 (SMX)] Where L leucine (C 6 H 13 NO 2 )symbolized (LeuH) as a primary ligand and Sulfamethoxazole C 10 H 11 N 3 O 3 S) symbolized (SMX)) as a secondary ligand . The ligands and the metal chlorides were brought in to reaction at room temperature in(v/v) ethanol /water as solvent containing NaOH. The reaction required the following [(metal: 2(Na Leu --): (SMX )] molar ratios with M(II) ions, Were M ( Mn ( II),Co (II),Ni(II),Cu( II),Zn (II),Cd(II)and Hg( The UV Vis and magnetic moment data revealed an octahedral geometry around M(II), The conductivity data show a non electrolytic nature of the complexes . The
... Show MoreNew twin compounds having four-, five-, and seven- membered heterocyclic rings were synthesized via Schiff bases (1a,b) which were obtained by the condensation of o-tolidine with two moles of 4- N,N-dimethyl benzaldehyde or 4- chloro benzaldehyde. The reaction of these Schiff bases with two moles of phenyl isothiocyanate, phenyl isocyanate or naphthyl isocyanate as in scheme(1) led to the formation of bis -1,3- diazetidin- 2- thion and bis -1,3- diazetidin -2-one derivatives (2-4 a,b). While in scheme (2) bis imidazolidin-4-one (5a,b) ,bistetrazole (6a,b) and bis thiazolidin-4-one (7a,b) derivatives were produced by reacting the mentioned Schiff bases(1a,b)with two moles of glycine, sodium azide or thioglycolic acid, respectively. The new b
... Show MoreIn this study, a new Azo ligand 5-((2-(1H-indol-2-yl)ethyl)diazinyl)-2-aminophenol is synthesized from a reaction of Tryptamine with 2-aminophenol. The ligand and their metal ion complexes Ni(II), Pd(II) , Pt(IV) and Au(III) have been synthesized and characterized by various analytical techniques, including elemental microanalysis, metal content, chloride-containing, measurement of electrical conductivity, magnetic susceptibility, 1H and 13C-NMR, FT-IR, UV-Vis, mass spectra (MS), and thermal analysis (TGA and DSC) curves. The DCS curve was used to calculate the thermodynamic parameters ΔH, ΔS, and ΔG. The characterization results promote the metal complexes of azo ligand structures. The results indicate that the
... 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
The reaction of 2-amino benzoic acid with 1,2-dichloroethane under reflux in methanol and KOH as a base to gave the precursor [H4L]. The precursor under reflux and drops of CH3COOH which reacted with (2mole) from salicycaldehyde in methanol to gave a new type N2O4 ligand [H2L], this ligand was reacted with (MCl2) Where [M= Co (II), Ni(II), Cu(II) and Zn(II)] in (1:1) ratio at reflux in methanol using KOH as a base, to give complexes of the general formula [M(L)]. All compounds have been characterized by spectroscopic methods [1H NMR ( just to the ligand), FTIR, uv-vis, atomic absorption], melting point, conductivity, chloride content, as well as m
... Show MoreThe reaction of 2-amino benzoic acid with 1,2-dichloroethane under reflux in methanol and KOH as a base to gave the precursor [H4L]. The precursor under reflux and drops of CH3COOH which reacted with (2mole) from salicycaldehyde in methanol to gave a new type N2O4 ligand [H2L], this ligand was reacted with (MCl2) Where [M= Co (II), Ni(II), Cu(II) and Zn(II)] in (1:1) ratio at reflux in methanol using KOH as a base, to give complexes of the general formula [M(L)]. All compounds have been characterized by spectroscopic methods [1H NMR ( just to the ligand), FTIR, uv-vis, atomic absorption], melting point, conductivity, chloride content, as well as magnetic susceptibility measurements. From the above data, the proposed molecular structu
... Show MoreThe ligand [Potassium (E)-(4-(((2-((1-(3-aminophenyl) ethylidene) amino)-4-oxo-1, 4-dihydropteridin-6-yl) methyl) amino) benzoyl)-L-glutamate] was prepared from the condensation reaction of folic acid with (3-aminoacetophenone) through Schiff reaction to give a new Schiff base ligand [H2L]. The ligand [H2L] was characterized by elemental analysis CHN, atomic absorption (AA),(FT-IR),(UV-Vis), TLC, ES mass (for spectroscopes), molar conductance, and melting point. The new Schiff base ligand [H2L], reacts with Mn (II), Co (II), Ni (II), Cu (II), Cr (III) and Cd (II) metal ions and (2-aminophenol),(metal: derivative ligand: 2-aminophenol) to give a series of new mixed complexes in the general formula:-K3 [M2 (HL)(HA) 2],(where M= Mn (II) and Cd
... Show MoreAllopurinol derivative were prepared by reacting the (1-chloroacetyl)-2-Hydropyrazolo{3,4-d}pyrimidine-4-oneiwith 5- methoxy- 2-aminoibenzothiazoleiunder certain conditions to obtain new compound ( N- (2-aminoacetyl (5-methoxy) benzothiazole -2yl) (A4), Reaction of 5-(P-dimethyl amine benzene)-2-amino-1,3,4- oxadiazole in the presence of potassium carbonate anhydrous to yield new compound (N-(2- aminoacetyl-5-(P-dimethyl amine benzene )-1,3,4-oxadiazoles-2-yl)(A30) and Azo compound (N-(5-(Azo-2-hydroxy-5-amino benzene)-1,3-Diazol-2yl)Allopurinol(A46). The structure of prepared compounds were confirmed by (FT-IR)
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