The purpose of this research is to prepare new vanillic acid derivatives with 1,2,4-triazole-3-thiol heterocyclic ring and evaluate their antimicrobial activity in a preliminary assessment. A multistep synthesis was established for the preparation of new vanillic acid-triazole conjugates. The intermediate of 4-(4-amino-5-mercapto-4H-1,2,4-triazol-3-yl)-2-methoxyphenol (4) reacts with different heterocyclic aldehydes (thiophene-2-carboxaldehyde, pyrrole-2-carboxaldehyde, thiophene-3-carboxaldehyde, and furfural ) in ethanol containing few drops of acetic acid yielded the corresponding 4-(4-(substituted amino)-5-mercapto-4H-1,2,4-1triazol-3-yl)-2-methoxy phenol derivatives (5-8). These compounds were characterized spectroscopically by FT-1IR and 1H-1NMR. These imine derivatives (5-8) were tested for their antimicrobial activity and compared with three different standard references (amoxicillin, ciprofloxacin, and fluconazole). Overall, compounds 6 and 8 exhibited varying degrees of inhibitory effects on the growth of the examined bacterial species and fungus. The most active one is compound 6 having pyrrole ring imine derivative showed potent activity against C. 1albicans and moderate activity against all tested bacteria compared to other derivatives but no activity toward P. 1aeruginosa and P. 1mirabilis.
With the aim of developing potential antimicrobials, a series of novel Ciprofloxacin methylene isatin derivatives incorporating different aromatic aldehydes were synthesized and characterized by FTIR, 1H NMR, Mass spectroscopy and bases of elemental analysis. In addition, the in vitro antibacterial and antifungal properties were tested against some human pathogenic microorganisms by employing the disc diffusion technique. A majority of compounds were showing activity against several of the microorganisms. The relationship between the functional group variation and the biological activity of the evaluated compounds is discussed. From comparisons of the compounds, 3c was determined to be the most active compound.
In search of novel antibacterial agent, a series of new isatin derivatives (3a-d) have been synthesized by condensation isatin (2,3-indolinendione) with piperidine (hexahydropyridine), hydrazine hydrate and Boc-amino acids respectively. Compounds synthesized have been characterized by IR spectroscopy and elemental analysis. In addition, the in vitro antibacterial properties have been tested against E. coli, P. aeruginosa, and Bacillus cereus, S. aureus by employing the well diffusion technique. A majority of the synthesized compounds were showing good antibacterial activity and from comparisons of the compounds, compound 3d has been determined to be the most active compound.
compound [1] was formed from the reaction of benzoin and benzaldehyde in the presence of ammonia, which was reacted with sodium hydride in DMF to obtain imidazole salt. This salt was reacted with adipoyl chloride to give compound [2]. Acid hydrazide derivative [3] was obtained from the reaction of compound [2] with hydrazine hydrate. After that Shiff bases [4-9] have been synthesized from the reaction of compound [3] with different aromatic aldehydes. These new formed compounds were diagnosed by 13C-NMR, 1H-NMR for some of them (in Ahl-Albate University in Jordan) and FT-IR spectroscopy (In Baghdad University). All of the prepared products have been studied their biological activities toward two kinds of bacteria. These products show
... Show Moren this study new derivatives of Schiff bases (5-10) were synthesized from the new starting material 1 . Which has been synthesized by the reaction of (1 mol.) of dichloroacetic acid with two moles of morpholine, in the presence of potassium hydroxide, Ester derivatives 2 and 3 were synthesized by the reaction of 1 with methanol or ethanol respectively in the presence of sulphuric acid as catalyst . Compound 2 was also prepared from dimethylsulphate with high yield , 2 and 3 was used to synthesized 2,2-dimorpholinylacetohydrazide 4 via reaction with NH2NH2.H2O 80% .Imines (5-10) were synthesized via the reaction of 4 with appropriate aromatic aldehydes in the presence of G.A.A as a catalyst . Derivatives compounds (1-10) were identifie
... Show MoreThe spectrum of clinical efficacy of Methotrexate (MTX) is broad in that MTX is used in the treatment of certain cancers, severe psoriasis and rheumatoid arthritis.Various mechanisms by which cancer cells grown in tissue culture become resistant to anticancer drugs. The use of multiple drugs with different mechanisms of entry into cells and different cellular targets allows for effective chemotherapy and high cure rates. In an efforts to develop effective strategies that increase the therapeutic potential of anticancer drugs with less systemic toxicity ,are being directed towards the investigation of dietary supplements and other phytotherapeutic agents for their synergistic efficacy in combination with anticancer drugs. A promi
... Show MoreThe spectrum of clinical efficacy of Methotrexate (MTX) is broad in that MTX is used in the treatment of certain cancers, severe psoriasis and rheumatoid arthritis.Various mechanisms by which cancer cells grown in tissue culture become resistant to anticancer drugs. The use of multiple drugs with different mechanisms of entry into cells and different cellular targets allows for effective chemotherapy and high cure rates. In an efforts to develop effective strategies that increase the therapeutic potential of anticancer drugs with less systemic toxicity ,are being directed towards the investigation of dietary supplements and other phytotherapeutic agents for their synergistic efficacy in combination with anticancer drugs. A pr
... Show MoreThis work includes preparation of Az, Qz, and Tz derivatives from the reaction of Schiff base (Sb) derivative with anthranilic acid, chloroacetyl chloride, and sodium azide, as well as, the characterization via FT-IR, 1H-NMR, and 13CNMR. The anticorrosion inhibition of these compounds was studied and the measurements of carbon steel (CS) corrosion in sodium chloride solution 3.5% (blank) and inhibitor in solutions were calculated at a temperature range of 293-323 K by the technique of electrochemical polarization. In addition, some thermodynamic and kinetic activation parameters for inhibitor and blank solutions (Ea⋇, ΔH⋇, ΔS⋇, and ΔG⋇) were determined. The results showed high inhibition efficacy for all the prepared compounds,
... Show MoreA total of 200 samples (180 fecal materials and 20 organ samples) were collected from (5 different poultry farms, 10 local poultry shops, 5 houses poultry, 5 Eggs stores shops and 5hand slaughters centers) in Ibb city, Yemen, 2014. According to morphological, cultural, as well as biochemical characterization and serological tests, 59(29.5%) isolates were identified as Salmonella spp. and all Salmonella isolates were categorized by serotype, which comprised of, 37(62.71%) Salmonella Typhimurium serovar, 21(35.59%). Salmonella Enteritidis serovar and 1(1.69%) Salmonella Heidlberg serovar. Antibiotic sensitivity test was done for bacterial isolates and the results showed there were clear differences in antibiotic resistant. Antimicrobial
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