A new Schiff base [I] was prepared by refluxing Amoxicillin trihydrate and 4-Hydroxy- 3,5-dimethoxybenzaldehyde in aqueous methanol solution using glacial acetic acid as a catalyst. The new 1,3-oxazepine derivative [II] was obtained by Diels- Alder reaction of Schiff base [I] with phthalic anhydride in dry benzene. The reaction of Schiff base [I] with thioglycolic acid in dry benzene led to the formation of thiazolidin-4-one derivative [III]. While the imidazolidin-4-one [IV] derivative was produced by reacting the mentioned Schiff base [I] with glycine and triethylamine in ethanol for 9 hrs. Tetrazole derivative [V] was synthesized by refluxing Schiff base [I] with sodium azide in dimethylformamid DMF. The structure of synthesized compounds[I-V] was characterized by their melting points, elemental analysis CHN-S and by their spectral data; FTIR and 1H NMR spectroscopy. Two cancer cell lines include: (RD) human pelvic rhabdomyosarcoma and (L20B) the mice intestines carcinoma cell line (which expresses the genes for human cellular receptor for Polio viruses) were used in this study. The cytotoxic effect of different concentrations of all the synthesized compounds for 48 hrs was examined. All compounds except [IV] and [V] showed less than 50% inhibition for (L20B), while these compounds exhibit inhibition more than 50% inhibition for (RD).
This work comprises the synthesis of new thioxanthone derivatives containing C-substituted thioxanthone. To obtain these derivatives, the o-mercapto benzoic acid was chosen as the starting material, which was reacted with dry benzene in sulfuric acid (98 %) to produce the thioxanthone (1). The 2,7-(disulfonyl phosphine imine) thioxanthone (4-8) were prepared from reaction of compound (1) with chlorosulfonic acid gave 2,7-(disulfonyl chloride) thioxanthone (2). Treatment of (2) with sodium azide to produce 2,7-(disulfonyl azide) thioxanthone (3). Condensation of (3) with phosphorus compounds afforded compounds (4-8). The 2,7-(disulfonamide) thioxanthone (9-21) was obtained when co
... Show MoreThis work comprises the synthesis of new phenoxazine derivatives containing N-substituted phenoxazine starting from phenoxazine (1). Synthesis of ethyl acetate phenoxazine (2) through the reaction of phenoxazine with ethylchloroacetate, which reacted with hydrazine hydrate to give 10-aceto hydrazide phenoxazine (3), then reacted with formic acid to give 10-[N-formyl acetohydrazide] phenoxazine (4). Reaction of compound (4) with phosphorous pentaoxide or phosphorus pentasulphide to gave 10-[N-methylene-1,3,4-oxadiazole] phenoxazine (5) and 10-[N-methylene-1,3,4-thiadiazole] phenoxazine (6).
This work includes synthesis of new phenoxazine derivatives containing N-substituted phenoxazine starting from phenoxazine (1).10-nitrosyl phenoxazine was prepared through the reaction of phenoxazine with sodium nitrite to give compound (2), which reacted with zinc in acetic acid to give 10-amino phenoxazine (3). Condensation of compound (3) with benzoyl chloride, isovaleryl chloride and 4-bromophenacyl chloride gave 10-amido phenoxazine derivatives (4-6).
In this work two moles of 2-amino benzothiazole were allowed to react with one mole of pyromellitic dianhydride to produce N,N‾-Bis-(benzathiazol-2-yl) pyromellitamic diacid [I] which was submitted to esterification via the reaction with dimethyl sulphate in sodium carbonate in acetone as a solvent to synthesize N,N‾-bis-(benzothiazol-2-yl) pyromellitam diacetate [II] .This ester was used to produce novel compounds through two paths :- Path one:- Reaction of ester [II] with hydrazine in ethanol as a solvent to form the corresebonding N,N‾-bis (benzothiazole-2-yl) –pyromellitamic acid hydrazide [III] which react with acetyl acetone in ethanol or with phthalic anhydride in dioxa
... Show MoreColorectal cancer (CRC) is the most common disease and cause of death globally. The aim of the study is investigation and detection of some bacterial interfering with CRC occurrence and progression. The study conducted between September 2022 till February 2023, a total of 50 specimens were collected from confirmed CRC patients. In addition, 50 stool specimens were collected from Healthy volunteers, considers as control group. Isolation and identification of bacteria in all collected specimens were done by using cultural and differential media (blood agar, macconkey agar and Pfizer agar), as well as the VITEK- 2 compact system. The bacterial species, in the specimens of control were ( Escherichia coli 50 (86.20%), Klebsiella Pneumoni
... Show MoreQuantitative real-time Polymerase Chain Reaction (RT-qPCR) has become a valuable molecular technique in biomedical research. The selection of suitable endogenous reference genes is necessary for normalization of target gene expression in RT-qPCR experiments. The aim of this study was to determine the suitability of each 18S rRNA and ACTB as internal control genes for normalization of RT-qPCR data in some human cell lines transfected with small interfering RNA (siRNA). Four cancer cell lines including MCF-7, T47D, MDA-MB-231 and Hela cells along with HEK293 representing an embryonic cell line were depleted of E2F6 using siRNA specific for E2F6 compared to negative control cells, which were transfected with siRNA not specific for any gene. Us
... 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 MoreAmoxicillin 1 was treated with thiosemicarbazide and Phosphoryl chloride to obtain a new derivatives that contains 1,3,4-thiadiazole moiety 2. Schiff bases compounds were synthesized by the reaction of compound 2 with different aldehydes such as benzaldehyde and some substituted Benzaldehyde; p-hydroy, p-Chloro, p-Nitro, p-Dimethylamino, p-Methyl, p-Methoxy, p-Ethoxy to give compounds 3a-h. The obtained compounds have tested towards gram -ve and gram +ve bacteria. The compound shows good to moderate result towards the bacteria.
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 MoreNew 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.