This research includes the synthesis of some new different heterocyclic derivatives of 5-Bromoisatin. New sulfonylamide, diazine, oxazole, thiazole and 1,2,3-triazole derivatives of 5-Bromoisatin have been synthesized. The synthesis process started by the reaction of 5-Bromoisatin with different reagents to obtain schiff bases of 5-Bromoisatin intermediate compounds(1, 8, 19) by using glacial acetic acid as a catalyst in three routes. The first route, 5-Bromoisatin reacted with p-aminosulfonylchloride to product compound(1), then converted to sulfonyl amide derivatives(2-7) by the reaction of compound(1) with different substituted primary aromatic amine in absolute ethanol. The second route includes the reaction of 5-Bromoisatin reacted with ethyl glycinate to give 5-bromo-3-(Ethyl imino acetate)-2-oxo indole(8), which undergo react with hydrazine hydrate 80% to obtain hydrazine derivatives(9) that react with different acid anhydrides to obtain diazine derivatives(10-14). Also compound(8) reacts with urea and thiourea to give compounds(15,16) which undergo cyclization with p-bromophenacylbromide in absolute ethanol as a solvent to obtain oxazole (17) and thiazole (18), respectively. The third route included the reaction of 5-Bromoisatin with p-phenylenediamine in ethanol to obtain compound(19) which is converted to new substitutes 1,2,3-triazole derivatives(22,23) by diazotation of compound(19) and treating the resulted salt(20) with sodium azid, then acetylaceton or ethylacetoacetate, respectively. Newly synthesized compounds were identified by spectral methods. (FTIR, 1H-NMR, 13C-NMR) and measurements of some of its physical properties and also some specific reactions. Furthermore the effects of the synthesized compounds were studied on some strains of bacteria.
In this research, 5- membered heterocyclic compounds as oxazolidine-5-one J1-J5 derivatives were prepared using primary aromatic amine, aromatic carbonyl compounds and chloroacetic acid. By combining primary aromatic amines and aromatic carbonyl compounds, Schiff's bases were synthesized. Schiff bases are used with the chloroacetic acid compound to prepare oxazolidine-5-one J1-J5 derivatives. The compounds J1-J5 were described using NMR spectroscopy and FT-IR. .The biological efficacy was evaluated according to maximum inhibitory concentrations (MICs) toward Staphyloccoccus aureus and Esherichia coli. The best MIC was 210 μg ml-1 for J4 against the two pathogenic bacteria, while J1, J4, and J1 did not show any inhibitory effect against all
... Show MoreThis search include the synthesis of some new 1,3-oxazepine derivatives have been prepared, starting from reaction of L-ascorbic acid with dry acetone in presence of dry hydrogen chloride afforded the acetal (I). Treatment of the latter with p-nitrobenzoyl chloride in dry pyridine yielded the ester (II) which was dissolved in (65%) acetic acid in absolute ethanol yielded the glycol (III). The reaction of the glycol (III) with sodium periodate in distilled water at room temperature produced the aldehyde (IV). The compound (V) [2-amino-5-mercapato-1,3,4-thiadiazole] was prepared through the reaction of thiosemicarbazide with carbon disulphide (CS2) in entity of anhydrous (Na2CO3) in (abs. ethanol ). Compound (VI) [2-(5-mercapto-1,3,4-thiadiaz
... Show MoreWith 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.
New schiff bases series (VIII) a-e and 1,3-thiazolidin-4-one derivatives (IX) a-e containing the 1,2,4-triazole and 1,3,4-thiazazole rings were synthesized and screening their biological activities. These compounds were identified via Fourier transform infrared (FT-IR) spectra, some via Proton nuclear magnetic resonance (1H-NMR) and mass spectra. The biological results indicated that all of these compounds did not reveal antibacterial effectiveness against (Escherichia coli and Klebsiella species) (G-). Some of these compounds showed moderate antibacterial activity against (Staphylococcus aureus, and Staphylococcus epidermidis) (G+), and all compounds exhibited moderate activity against Candida albicans.
In this research investigation, a total of eighteen diverse tetra- and penta-lateral cyclic compounds were synthesized. These included 1,3,4-thiadiazole, thiazolidin-4-one (via an alternative method), 1,2,4-triazole, carbothioamide, thiazole-4-one, azetidin-2-one, and oxazole. The synthesis procedure entailed a sequence of reactions. The thiazolidine-4-one 1 was obtained by reaction p-aminobenzoic acid with thiosemicarbazide, followed by treatment with p-tolualdehyde to produce Schiff base 2. Reaction Schiff base 2 with mercaptoacetic acid in dry benzene was carried out to produce thiazolidine-4-one 3. In another synthesis pathway, the esterification of p-nitro benzoic acid with ethanol in the presence of sulfuric acid was
... Show MoreCondensation of 1,2- dibromo ethane with para hydroxy benzoic acid gave 1,2-Ethane-bis- 4-oxybenzoic [1]. This Compound was converted with the thionyl chloride to give 1,2-Ethane-bis- 4-oxybenzoyl chloride [2]. Reaction of compound [2] with thiosemicarbizades gave 1,2-Ethanebis[4-oxybenzoyl-thiosemicarbazide] [3] and opteined 1,2-Ethane-bis[3-mercapto-5-phenoxy- 1,2,4-triazole] [4] from treatment compound [3] with NaOH (4%) .The new compounds 1,2- Ethane-bis[3-(substituted thioacyl)-4-(substituted acyl)-5 phenoxy-1,2,4-triazole] [5a-d] and 1,2- Ethane-bis[3-(substituted alkylthio)-5 phenoxy-1,2,4-trizole] [5e-f] derived from compound [4] were synthesized and characterized by physical and spectral data. All the compounds [4], [5a-d] and [5e-
... Show MoreSynthesis and study liquid crystalline properties of new compounds with terminal groups of amides ([III]a-c,[IV]a-c and [VI]n), alkoxy series[V]n or ester with azo linkage ([IX]a-c and[X]a-c) containing thaizole ring. These series were synthesized by many steps starting from 4- hydroxyacetophenone or 4-aminoacetophenone. The synthesized compounds were characterized using melting points, FTIR, C.H.N.S analysis and for some of them 1H NMR spectroscopy. The liquid crystalline properties were studied by hot stage polarizing microscopy and differential scanning calorimetry DSC. All compounds of series [III]a-c,[IV]a-c and compounds [V]n showed enantiotropic liquid crystal. While the series [VI]n showed nematic mesomorphism except [VI]8 did not s
... Show MoreNew compounds containing heterocyclic units have been synthesized. These compounds include 2-amino 5- phenyl-1,3,4-thiadiazole (1) as starting material to prepare the Schiff bases 2N[3-nitrobenzylidene -2 hydroxy benzylidene and 4-N,N-dimethyl aminobenzylidene] -5-phenyl-1,3,4-thiadiazole (2abc) , 2N[3-nitrophenyl, 2-hydroxyphenyl or 4-N,N-dimethylaminophenyl] 3-]2-amino-5-phenyl-1,3,4-thiadiazole]-2,3-dihydro-[1,3]oxazepine-benzo-4,7-dione] (3abc), 2N[3-nitrophenyl,2-hydroxyphenyl,4-N,N-dimethylaminophenyl]-3-[2-amino-5-phenyl-1,3,4-thiadiazole-2-yl]-2,3-dihydro-[1,3]oxazepine-4,7-dione[(4abc), 2-N-[3-nitrophenyl, 2-hydroxyphenyl or 4-N,N-dimethylaminophenyl]-3-[2-amino-5-phenyl-1,3,4-thiadiazole-2yl]-1,2,3-trihydro-benzo-[1,2-e][1,3] diaz
... Show MoreThe organic compound imidazole has the chemical formula C3N2H4. Numerous significant biological compounds contain imidazole. The amino acid histidine is the most prevalent. The substituted imidazole derivatives have great potential for treating a variety of systemic fungi infections. Thiourea is an organosulfur compound with the formula SC(NH2)2. It is a reagent in organic synthesis. In this paper, some new imidazole and thiourea derivatives are synthesized, characterized, and studied for their biological activity. These new compounds were synthesized from the starting material terephthalic acid, which was transformed to corresponding ester [I] by the refluxing of diacid with methanol in the presence of H2SO4 as a catalyst, compound [I] con
... Show MoreA theoretical and protection study was conducted of the corrosion behavior of carbon steel surface with different concentrations of the derivative (Quinolin-2-one), namly (1-Amino-4,7-dimethyl-6-nitro-1H-quinolin-2-one (ADNQ2O)). Theoretically, Density Functional Theory (DFT) of B3LYP/ 6-311++G (2d, 2p) level was used to calculate the optimized geometry, physical properties and chemical inhibition parameters, with the local reactivity to predict both the reactive centers and to locate the possible sites of nucleophilic and electrophilic attacks, in vacuum, and in two solvents (DMSO and H2O), all at the equilibrium geometry. Experimentally, the inhibition efficiencies (%IE) in the saline solution (of 3.5%) NaCl were studied using potentiomet
... Show More