Objective: Benzoxazole derivatives have antifungal, anticancer, antibacterial, and anticonvulsant function. Encouraged by this comment, we agreed to synthesize new Benzoxazole compounds connected to the bases of Schiff's. Methods: 2,4-diaminophenol (1) was prepared by the reaction of 2,4-dinitrophenol and sodium dithionate. Compound (1) reacted with either acetic acid to afford compound (2) or with formic acid to afford compound (3). The Schiff bases were preparation from the reaction condensing reaction of compound (2) or (3) and aromatic aldehydes or ketone; [p-nitrobenzaldehyde, p-hydroxybenzaldehyde, p-chlorobenzaldehyde, p-bromoacetophenone and terephthaldehyde]. Results: FTIR and 1H-NMR spectroscopy characterized all of the preparation compounds. The synthesized derivatives against (Gram positive bacteria GPB) (Bacillus subtilis) and two (Gram-negative bacteria GNB) (Klebsiella pneumoniae and Escherichia coli) and (one fungal species Candida albicans), have been evaluated to their antibacterial activity in vitro. all results showed which most of them have good antibacterial activity, while their antifungal activity revealed that compounds displayed slight antifungal activity. The synthesized Benzoxazole derivatives were docked using, glucosamine 6-phosphate synthase as a ligand. Conclusion: The antimicrobial activity indicates that compounds (4), (7) and (8) have more potent antibacterial activity than the compounds (5) and (6). Molecular docking study revealed that compounds (7) and (8), with bulky phenyl groups are essential to block the active centers of (GluN-6-Ps) amino acids synthase in the bacteria.
Amoxicillin 1 was treated with thiosemicarbazide and Phosphoryl chloride to obtain a new derivatives that contains 1,3,4-thiadiazole moiety 2. Schiff bases compounds were synthesized by the reaction of compound 2 with different aldehydes such as benzaldehyde and some substituted Benzaldehyde; p-hydroy, p-Chloro, p-Nitro, p-Dimethylamino, p-Methyl, p-Methoxy, p-Ethoxy to give compounds 3a-h. The obtained compounds have tested towards gram -ve and gram +ve bacteria. The compound shows good to moderate result towards the bacteria.
Abstract
Nano-crystalline ZSM-5 zeolite was synthesized by hydrothermal method using chelating agent and two gel compositions:Compositionɪ:Al2O3:86SiO2:5.5TPA:12.7Na2O:3.4Trien:3320H2O.Compositionɪɪ:Al2O3:68SiO2:5.4TPA:10Na2O:2.6Trien:2626H2O.Study of hydrothermal reaction factors on characteristics of nano- sized zsm-5 has been carried on ,among them are crystallization temperature, crystallization time and concentration of template ( TPAOH ) solution. Synthesis was accomplished in PTFE lined autoclave ( reactor ) . The product were characterized by X-ray diffraction ( XRD ),Atomic force microsc
... Show MoreNew Schiff bases derivatives [IV]a-e is prepared via condensation of Derythroascorbic acid with p-substituted aldehydes in dry benzene. To obtain these derivatives, the 5,6-O-isopropylidene-L-ascorbic acid[I] was chosen as starting material, compound prepared from the reaction of L-ascorbic acid as starting material. Compound[I] was prepared from the reaction of L-ascorbic acid with dry acetone in the presence of hydrogen chloride. The esterification of hydroxyl groups at C-2 and C-3 positions with excess ofethyl α –chloroacetate in the presence of sodium acetate produce acorresebonding ester [II] , which was condensed with hydrazine hydrate to give new hydrazide [III] . The new Schiff bases [IV]a-e were synthesized by reaction of acid h
... Show More1,3,4-oxadizole and pyrazole derivatives are very important scaffolds for medicinal chemistry. A literature survey revealed that they possess a wide spectrum of biological activities including anti-inflammatory and antitumor effects.
To describe the synthesis and evaluation of two classes of new niflumic acid (NF) derivatives, the 1,3,4-oxadizole derivatives (compounds 3 and (4A-E) and pyrazole derivatives (compounds 5 and 6), as EGFR tyrosine kinase inhibitors in silico and in vitro.
The designed compounds were synthesized using convent
In study of effective bioactive compounds, we have synthesized the Co((ІІ), Mn(ІІ), Fe(ІІ), Cu(ІІ), Ni(ІІ), and Zn(ІІ) complexes of the Schiff base derived from trimethoprim and2'-amino-4-chlorobenzophenone and characterized by spectroscopic (NMR, IR, Mass, UV–vis,), analytical, TGA studies and magnetic data .The solution electronic spectral study suggests the stoichiometry of the synthesized complexes and Elemental analysis detected the square planer and octahedral geometry of the compounds. The prepared metal complexes presented promoted efficiency versus the screened bacterial (Escherichia Coli and Staphylococcus aureus) antibacterial efficacy against (Staphylococcus aureus, Salmonella spp., E. coli, Vibrio spp., Pseud
... Show MoreEight new complexes with the general formula [M(L)2(H2O)2] were prepared resulting from the reaction of the new Schiff base ligand [(E)-5- ((2-hydroxybenzylidene)amino)-2-phenyl-2,4-dihydro-3H-pyrazol-3- one(L)] with metal ions [manganese, cadmium, zinc, copper, nickel, cobalt, Mercury Bivalent and tetravalent platinum. This ligand was derived from the reaction of the amine (5-amino-2-phenyl-2,4-dihydro3H-pyrazol-3-one) with Salicylaldehyde, which is linked to the metal ions via two atoms. The nitrogen is the isomethene group, and the oxygen is the hydroxide group of the pyrazoline ring. The prepared compounds were characterized using infrared spectroscopy, nuclear magnetic resonance spectroscopy, and ultraviolet spectroscopy, and from the
... Show MoreThe aim of this work is the synthesis of new Schiff base derived from PVA and Erythro-ascorbic acid derivative (pentulosono-ɣ-lactone-2,3-enedianisoate) and its metal complexes of biological significance. All synthesized compounds were characterized by Thin layer chromatography (TLC) and FTIR spectra and aldehyde was also characterized by (U.V-Vis), 1HNMR, 13CNMR and mass spectra. The synthesized Schiff base & its metal complexes were screened for their in vitro antimicrobial activity against five pathogenic bacteria (Escherichia coli, Shigella dysentery,Klebsiellapneumonae,Staphylococcusaureus, Staphylococcus Albus) and two fungal (Aspergillus Niger,Yeast).The biological activity ofall complexes is higher than free Schiff base ligand andf
... Show MoreThe reaction of 2-amino-benzothiazole with bis [O,O-2,3,O,O – 5,6 – (chloro(carboxylic) methiylidene) ] – L – ascorbic acid (L-AsCl2) gave new product 3-(Benzo[d]Thaizole-2-Yl) – 9-Oxo-6,7,7a,9-Tertrahydro-2H-2,10:4,7-Diepoxyfuro [3,2-f][1,5,3] Dioxazonine – 2,4 (3H) – Dicarboxylic Acid, Hydro-chloride (L-as-am)), which has been insulated and identified by (C, H, N) elemental microanalysis (Ft-IR),(U.v–vis), mass spectroscopy and H-NMR techniques. The (L-as am) ligand complexes were obtained by the reaction of (L-as-am) with [M(II) = Co,Ni,Cu, and Zn] metal ions. The synthesized complexes are characterized by Uv–Visible (Ft –IR), mass spectroscopy molar ratio, molar conductivity, and Magnetic susceptibility techniques. (
... Show MoreHeterogeneous organic compounds play an important role in our daily life as they contribute in many medical and industrial fields and are in continuous development as a result of the preparation of new derivatives with different properties. From this premise, the goal of this work appears, which is preparation of (four, five, six, and seven) membered ring systems derived from furfural, by its reaction with different aromatic aldehydes, and record their antioxidant activity by using free radical scavenging method of DPPH radicals. The new ring systems are synthesized by reacting the prepared Schiff-bases with different ring closure agents (chloroacetyl chloride, mercaptoaceticacid, anthranilic acid, and phthalic anhydride), the prep
... Show More