This research includes the synthesis of new series of heterocyclic compounds. Reaction of 2-nitro benzylidene)thiosemicarbazide(1) with ethyl chloro acetate gave (2-nitro benzylidene amino)-2-thioxomidazolidine-4-one(2) ,treatment(2) with methyl iodide to give(3)which was reacted with hydrazine to give 2-hydrazinyl-1-[(2-nitrobenzylidene)amino]- 1H-imidazol-5(4H)-one, andreation of compound(2) with aromatic aldehydes to give 5arylidene -3-({2-nitro benzylidene}amino)2-thioxo-3,5-dihydro-4H-imidazole-4-one(5a,5b), which was reacted with ethyl aceto acetate to give 4-aryl-1-[2-nitrobenzylidene, amino -6oxo-2-thioxo octa hydro-1H-benzo[d]imidazole-5-carboxylate and followed synthesis of βlactamederivtives(9a,9b) by treatment derivatives(8a,8b)schiff bases with chloro acetyl chloride .some new compounds were characterized by of some protone NMR of them and IR spectroscopy.
Aim: To evaluate the cytotoxic activity of newly synthesized a series of novel HDAC inhibitors comprising sulfonamide as zinc binding group and Isatin derivatives as cap group joined by mono amide linker as required to act as HDAC inhibitors. Materials and Methods: The utilization of sulfonamide as zinc binding group joined by N-alkylation reaction with ethyl-bromo hexanoate as linker group that joined by amide reaction with Isatin derivatives as cap groups which known to possess antitumor activity in the designed of new histone deacetylase inhibitors and using the docking and MTT assay to evaluate the compounds. Results: Four compounds have been synthesized and characterized successfully by ART-FTIR, NMR and ESI-Ms. the compounds w
... Show MoreThe outstanding evidence of phthalimide pharmacophore in securing enhanced biological activities had encouraged further research and development into phthalimide-based derivatives as potential new drugs. In this study, phthalimide core was hybridized with aldehydes giving integrated imines displaying different types of functionalities and at alternating positions. The resulting compounds, therefore, provide an innovative window to explore possible differential biological effects as antioxidants and anticancer agents. A total of sixteen compounds were synthesized, and each was verified by FT-IR, H NMR, C NMR, and MS characterization. Herein, a facile single-step synthesis method was employed substituting the conventional two-step che
... Show MoreAbstract New derivatives of 1,2,4- triazole , 1,2,4-triazole -3-one and 1,2,4-triazole-3-thione were obtained through this research. Acid hydrazide derivative was present from reaction of poly acryloyl chloride with hydrazine hydrate in presence of DMF as a solvent then reacted with benzonitrile and its derivatives to give 1,2,4-triazole derivatives. After that reaction of poly acryloyl chloride with semicarbazide and semithiocarbazide to form semicarbazone and semithiocarbazone derivatives respectively. Finally, closing of semicarbazone and semithiocarbazone derivatives with 2% NaOH gave 1,2,4-triazole -3-one and 1,2,4-triazole-4-thione derivatives respectively. These new synthesized products have been characterized by infrared, 1 H-n
... Show MoreThe studies on the antiviral compound chalcone in vitro in both tissue and organ culture systems against rubella virus glass that this compound relatively non toxic to the cell culture and organ culture of the concentration of 8 ug/ml or less, chalcone have significantly antiviral activity against rubella virus in tissue culture and organ culture. We find that a concentration of 0.03ug/ml or more inhibit the IOOTCID50 of rubella virus. The therapeutic index (TI) used in this study to evaluate the drug, the (TI) which is the ratio of the dose of drug which is just toxic (Maximum tolerated dose) to the dose which is just effective (Minimum effective dose). If this index is one or less it not possible to use the drug under the conditions outli
... Show MoreThis 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 rea
... 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 MoreThis work includes the synthesis of some new five- seven heterocyclic rings derived from benzenesulfonylhydrazide as starting material. Its condensation with 4-methoxy and 4nitro benzaldehyde gives the Schiff bases (1a,b). Schiff bases were reacted with cyclic anhydrides given Oxazepine, Thiazepine derivatives(2,3,4 a,b)(seven membered ring) and with 2-mercapto benzoic acid gives thiazine derivatives (6a,b)(six membered ring) finally with thioglycolic acid give thiazolidine ring(five membered ring) scheme(3). The synthesized compounds have been characterized by melting points,FT-IR, 1H-NMR spectroscopy ,13CNMR and Elemental analysis. some of synthesized compounds were tested for their antibacterial activity
... Show MoreNew bidentate dithiocarbamate ligand (NaL) namely [Sodium-2-(((3-methyl -4- “(2,2,2-tri fluoro ethoxy) pyridin-2â€-yl) methyl) sulfinyl)-1H-benzoimidazole -1-carbodithioate] was prepared. This free ligand was synthesized from the reaction of a (RS)-2-([3-methyl -4-(2,2,2-tri fluoroethoxy) pyridin-2-yl] methyl sulfinyl)-1H benzoimidazole, CS2 and NaOH in methanol as solvent. From reaction of dithiocarbamate salt (NaL) with metal ions (M); Co(II), Ni(II), Cu(II), Zn(II), Cd(II) and Pd(II)â€, have obtained the DTC complexes at general molecular formula [M(L)2(H2O)2] and [Pd(L)2]. To characterize the ligand and its complexes, used different analyses methods such FTIR, UV-Vis, elemental microanalysis, atomic absor
... Show MoreNew bidentate dithiocarbamate ligand (NaL) namely [Sodium-2-(((3-methyl -4- “(2,2,2-tri fluoro ethoxy) pyridin-2”-yl) methyl) sulfinyl)-1H-benzoimidazole -1-carbodithioate] was prepared. This free ligand was synthesized from the reaction of a (RS)-2-([3-methyl -4-(2,2,2-tri fluoroethoxy) pyridin-2-yl] methyl sulfinyl)-1H benzoimidazole, CS2 and NaOH in methanol as solvent. From reaction of dithiocarbamate salt (NaL) with metal ions (M); Co(II), Ni(II), Cu(II), Zn(II), Cd(II) and Pd(II)”, have obtained the DTC complexes at general molecular formula [M(L)2(H2O)2] and [Pd(L)2]. To characterize the ligand and its complexes, used different analyses methods such FTIR, UV-Vis, elemental microanalysis, atomic absoreption, magnetic susceptibil
... Show MoreFour metal complexes mixed ligand of 2-aminophenol (2-AP) and tributylphosphine (PBu3) were produced in aqueous ethanol with (1:2:2) (M:2-AP:PBu3). The prepared complexes were identified by using flame atomic absorption, FT.IR and UV-Vis spectroscopic methods as well as magnetic susceptibility and conductivity measurements. In addition antibacterial activity of the two ligands and mixed ligand complexes oboist three species of bacteria were also examined. The ligands and their complexes show good bacterial activities. From the obtained data the octahedral geometry was suggested for all prepared complexes.