A series of novel hybrid molecules containing 1,3,4-oxadiazole and 1,3,4-thiadiazole moieties bearing an ibuprofen moiety were designed, synthesized, and evaluated for their in vitro antibacterial activity against Gram-positive and Gram-negative bacteria. A carboxylic acid compound with a 1,3,4-thiadiazole unit was synthesized via the coupling reaction of 5-(1-(4-isobutylphenyl) ethyl)-1,3,4-thiadiazol-2-amine with benzoic acid. This compound was then used as the starting material to make several new 1,3,4-oxadiazole derivatives through ring closure reactions, after first converting it to its ester (methyl 4-(5-(1-(4-isobutylphenyl)ethyl)-1,3,4-thiadiazol-2-yl) benzoate) and then to the acid hydrazide (4-(5-(1-(4-isobutylphenyl) ethyl)-1,3,4-thiadiazol-2-yl)benzohydrazide). Finally, the intramolecular ring closure of the hydrazide compound with carboxylic acids under reflux in POCl₃ afforded 2-(4-(5-(1-(4-isobutylphenyl)ethyl)-1,3,4-thiadiazol-2-yl)phenyl)1,3,4-oxadiazole derivatives. The synthesized compounds were characterized using spectroscopic techniques, including IR, ¹H NMR, and ¹³C NMR. The compounds were tested for antibacterial activity on two Gram-positive (Streptococcus pyogenes and Staphylococcus aureus) and two Gram-negative (Escherichia coli and Proteus mirabilis) bacterial strains. The prepared compounds demonstrated significant antibacterial activity compared with Ibuprofen and Ampicillin. The maximum inhibition zones were recorded against Staphylococcus aureus (20 mm), Proteus (18 mm), Escherichia coli (17 mm), and Streptococcus (17 mm), suggesting that the synthesized derivatives possess promising antibacterial properties. This difference resulted from substituting the benzene ring with various substituents.
A small number of researches were done in the design and synthesis of enkephalin analogues that are able to resist degradation effect of proteolytic enzymes with good bioavailability and half-lives.Through studying structure activity relationships we tried to incorporate phthalyl group, tryptophan and lysine amino acids in different positions in the basic backbone structure of the naturally occurring opioid Leu5- and Met5- enkephalin, in the hope that such insertion of these amino acids could induce interesting addition in the biological activity of these analogues with enhancement of their bioavailability, in addition to decrease side effects as addiction liability.
These synthesized peptides are:
In this research, cyclic compounds derived from 2- furfural mercaptan (oxazole, triazoles) were synthesized, and their biological efficacy was measured and compared with standard drugs. Also, their effectiveness as anti-oxidant was measured and compared with ascorbic acid as a standard substance. Some of the synthesized compounds were deduced with good efficacy. © 2021 Sami Publishing Company. All rights reserved
The synthesis of new substituted cobalt Phthalocyanine (CoPc) was carried out using starting materials Naphthalene-1,4,5, tetracarbonic acid dianhydride (NDI) employing dry process method. Metal oxides (MO) alloy of (60%Ni3O4 40%-Co3O4 ) have been functionalized with multiwall carbon nanotubes (F-MWCNTs) to produce (F-MWCNTs/MO) nanocomposite (E2) and mixed with CoPc to yield (F-MWCNT/CoPc/MO) (E3). These composites were investigated using different analytical and spectrophotometric methods such as 1H-NMR (0-18 ppm), FTIR spectroscopy in the range of (400-4000cm-1), powder X-rays diffraction (PXRD, 2θ o = 10-80), Raman spectroscopy (0-4000 cm-1), and UV-Visib
... 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 MoreThe current work reports a new Schiff base [N1-benzylidenebenezene-1,2-diamine(L) = C20H16N2] has been synthesized from benzaldehyde (C6H5CHO) and O- aminoaniline (O-C6H4(NH2)2. Metal mixed ligand complexes of the Schiff base were prepared from chloride salts of Zn(II), Cd(II) and Hg(II) in ethanol and 8-hydroxyquinoline(8HQ)(C9H7NO) containing sodium hydroxide. All the complexes were characterized on the basis of their; FT-IR and U.V spectra, melting point, molar conductance, and determination of the percentage of the metal in the complexes by flame (AAS). In the all complexes, (8HQ) behaves as a bidentate ligand as primary ligand through –-OH phenolic group and –N groups of pyridine group. Also, the prepared ligand (L) was bidentate i
... Show MoreThe reaction paths of the C-C and C-H bond cleavage in the anthracene and phenanthrene aromatic molecules are studied by applying the ab-initio DFT method. It is found that the C-C bond cleavage proceeds via a singlet aromatic transition state, compelled through a disrotatoric ring opening reaction. A suprafacial H atom shift follows the transition state, leading to the formation of a methylene -CH2 and an acetylenic or allenic moiety. The calculated activation energies for anthracene range from 158.81-208.90 kcal/mol and the reaction energies from 96.106-156.976 kcal/mol. For phenanthrene, the energy values are 157.39-202.34 kcal/mol and 62.639-182.423 kcal/mol, respectively. For the C-H cleavage reactions, the calculated reaction energies
... Show MoreIn-vitro biological activities of the free new H4L ( indole-7-thiocarbohydrazone) ligand and its Ni(II), Pd(II) , Pt(II), Cu(II), Ag(I), Zn(II) and Cd(II) complexes are screened against two cancerous cell lines, that revealed significant activity only for [Cu2Cl2(H4L)2(PPh3)2] after 72 h treatment by the highest tested concentrations. The Copper(I) complex was characterized by X-ray Crystallography and the NMR spectra, whereas it has been confirmed to have momentous cytotoxicity against ovarian, breast cancerous cell lines (Caov-3, MCF-7). The apoptosis-inducing properties of the Cu(I) complex have been investigated through fluorescence microscopy visualization, DNA fragmentation analysis and propidium iodide flow cytometry.
This work includes the synthesis and identification of ligand {3-((4-acetylphenyl)amino)-5,5-dimethylcyclohex2-en-1-one} (HL* ) by the treatment of 5,5-dimethylcyclohexane-1,3-dione with 4-aminoacetophenone under reflux. The ligand (HL* ) was identified via FTIR, Mass spectrum, elemental analysis (C.H.N.), 1H and 13C-NMR spectra, UV-Vis spectroscopy, TGA and melting point. The complexes were synthesized from ligand (HL* ) mixed with 3-aminophenol (A) and metal ion M(II), where M(II) = (Mn, Co, Ni, Cu, Zn and Cd) at alkaline medium to produce complexes of general formula [M(L* )(A)] with (1:1:1) molar ratio. These complexes were detected via FT-IR spectra, UV-Vis spectroscopy as well as elemental analysis (A.A) and melting point, conductivit
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