The present work involved synthesis of serval new substituted tetrazole via Schiff bases for trimethoprim drug by two steps. The first step involved direct reaction of different ketones and aldehydes with trimethoprim producing the corresponding Schiff bases (1-10), whereas the second step, involved preparation new tetrazoles derivatives (11-20) through reaction of the ready Schiff bases (in the first step) with sodium azidein in dioxin. The prepared compounds were characterized by UV, FT-IR, and some of them by 13C-NMR, 1H-NMR spectroscopy and physical properties.
This work involves synthesis and characterization of some new 1, 3, 4-thiadiazole or pyrazoline derivatives heterocyclic containing indole ring. The new 2-amino-1, 3, 4-thiadiazole derivatives [IV] and [V] a, b were synthesized by cyclization reaction of 2-methyl-1H-indole-carbothiosemicarbazide [III] in H2SO4 acid or by reaction of indole-3-acetic acid or indole-3-butanoic acid with thiosemicarbazide in the presence of phosphorous oxychloride, respectively. Amide derivatives [VI]-[VIII] were synthesized by the reaction equimolar of 2-amino-1, 3, 4-thiadiazoles and (acetyl chloride, benzoyl chloride, anisoyl chloride and heptanoyl chloride) in DMF and pyridine as accepter. The new pyrazolone derivatives [XI] a, b were synthesized from heati
... Show MoreGold nanoparticles AuNPs have proven to be powerful tools in various nanomedicine applications, because of their photo-optical distinctiveness and biocompatibility. Noble metal gold nanoparticles was prepared by pulsed laser ablation method (1064-Nd: YAG with various Laser power from 200 to 800 mJ and 1 Hz frequency) in distil water. The process was characterized using UV-VIS absorption spectroscopy. Morphology and average size of nanoparticles were estimated using AFM and X-ray diffraction (XRD) analysis which show the nature of gold nanoparticles (AuNPs). Antibacterial activity of gold nanoparticles as a function of particles concentration against gram negative bacterium Escherichia coli and gram positive bacterial Staphylococcus aureu
... Show MoreA niger, a fungus which doesn't have high ability to production lipid, this fungus has been select to investigate the non oleaginicity. In this search, there are explorations about: i) growth profile ii) enzymes profile iii) isoforms. Growth profile shows that this fungus doesn't have ability to accumulate lipid more than 6% while bio mass are around 10g/l in spite of the presence of glucose in the media till the end of cultivation time and excision of nitrogen within 24 hrs. In enzyme study, we investigate all lipogenic enzymes Malic enzyme (ME), Fatty acid synthase (FAS), ATP: Citrate lays (ACL), NAD+ isocitrate dehydrogenase (NAD+ICDH), Glucose-6-phosphate (G6PD), and 6-phosphogluconate dehydrogenase (6PGD), all these enzymes show, ac
... Show MoreNew substituted anthraquinones with amino derivations fragments were synthesized through the substitution of bromine atom by different amines using the Ullmann coupling reaction. Obtained compounds based on anthraquinone used for experimental antimicrobial studies. The structure of the synthesized compounds was confirmed by LC-MS and 1H, 13C NMR spectroscopy. Studies on planktonic microorganisms have shown that the first synthesized anthraquinone derivatives have an inhibitory effect against bacteria and fungi. The triazene 1-(3-(benzoic acid(triaz-1-en-1-ol(-4-(1H-imidazol-1-yl(-9,10-dioxo-9,10-dihydroanthracene -2-sulfonic acid, have wide spectrum of activity, growth retardation zones against gram-positive micro
... Show MoreBackground: Frovatriptan succinate (FVT) is an effective medication used to treat migraines; however, available oral formulations suffer from low permeability; accordingly, several formulations of FVT were prepared. Objective: Prepare, optimize, and evaluate FVT-BE formulation to develop enhanced intranasal binary nano-ethosome gel. Methods: Binary ethosomes were prepared using different concentrations of phospholipid PLH90, ethanol, propylene glycol, and cholesterol by thin film hydration and characterized by particle size, zeta potential, and entrapment efficiency. Furthermore, in-vitro, in-vivo, ex-vivo, pharmacokinetics, and histopathological studies were done. Results: Regarding FVT-loaded BE, formula (F9) demonstrated the best paramet
... Show MoreIn this work 5-methylene-yl - (2-methy –oxazole-4-one) (1H) imidazole (1) were synthesized from the reaction of L-Histidine with acetic anhydride and which converted to the of 5-methylene-yl-(2-methyl 3-amino imidazole-4-one)-1H-imidazole (2) by reaction with hydrazine hydrate. Schiff bases (3-6) were synthesized from the reaction of compound (2) with different aromatic aldehyde. Reaction of compounds (3-6) with chloroacetyl chloride gives azetidinone one derivatives (7-10). These compounds were characterized by FT-IR and some of them with 1H-NMR and 13C-NMR spectroscopy.
The reaction of(2-oxo-2H-chromen-3-Carbonyl chloride)(k1) with hydrazine in boiling ethanol gives the hydrazide(K2).When compound (k2) reacts with various aromatic aldehydes ,the corres ponding Schiff bases(k3–k4) achieve new series of thiazotidines (k5–k6) and azetidinones (k7–k8) obtained from the reactions of appropriate Schiff bases with mercapto acetic acid and chloro acetyl chloride respectively. All the compounds are characterized by FT-IR,1H-NMR and GC-Ms.
New Derivatives for Known P- Jactam antibiotics were
synthesized utilizing the free amino group pres nt in the parent compounds as the site for derivatization. The objectives for this study
are to have new compounds which could have an increased potential resistance to the degradative enzymes knowing to be able to destroy
the antibacterial activity of 13· lactam antibiotics- Besides. these new
derivatives could be congeners of known agents, or may be a
pott:ntial pro-drugs for thes
... Show More