This work involves the preparation of the ligand [KL] :- ÂÂÂÂÂÂ
K[4-(N-(5-methylisoxazol-3-yl) sulfamyl) phenylcarbamodithioate] from the reaction of sulfamethoxazole with Carbon disulfide in the presence of potassium hydroxide under reflux (4 hours) using methanol as asolvent. The prepared ligand was characterized using FT-IR, UV-Vis, 1H,13C–NMR spectroscopy, molar conductivity and melting point, Complexes for the above ligand [KL] with some bivalent transition and non-transition metals (Mn +2, Co+2 , Ni+2 ,
... Show MoreThe prostaglandins inside inflamed tissues are produced by cyclooxygenase-2 (COX-2), making it an important target for improving anti-inflammatory medications over a long period. Adverse effects have been related to the traditional usage of non-steroidal anti-inflammatory drugs (NSAIDs) for the treatment of inflammation, mainly centered around gastrointestinal (GI) complications. The current research involves the creation of a virtual library of innovative molecules showing similar drug properties via a structure-based drug design. A library that includes five novel derivatives of Diclofenac was designed. Subsequently, molecular docking through the Glide module and determining the binding free energy implementing the P
... 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.
A new class of biologically active nanocomposites and modified polymers based on poly (vinyl alcohol) (PVA) with some organic compounds [II, IV, V and VI] were synthesized using silver nanoparticles (Ag-NPs). All compounds were synthesized using nucleophilic substitution interactions and characterized by FTIR, DSC and TGA. The biological activity of the modified polymers was evaluated against: gram (+) (staphylococcus aureus) and gram (-): (Es cherichia coli bacteria). Antimicrobial films are developed based on modified poly (vinyl alcohol) MPVA and Ag-NPs nanoparticles. The nanocomposites and modified polymers showed better antibacterial activities against Escherichia coli (Gram negative) than against Staphyloc
... Show MoreNon-steroidal anti-inflammatory drugs (NSAIDs) contain free –COOH which thought to be responsible for the GI irritation associated with all traditional NSAIDs. The esterification of this group is one of an approach to ultimate aim for reduce the gastric irritation; so in this study we synthesized and preliminarily evaluated new ester compounds as new analogues with expected selectivity toward COX-2 enzyme. Synthetic procedures have been successfully developed for the generation of the target compounds (III a and b). The synthetic approach involved multi-steps procedures which include: Synthesis of 4-hydroxy benzene sulphonamide ( I b ), synthesis of Naproxen and Ibuprofen acyl chloride and then reacting them with 4-hydroxy benzene sulphon
... Show MoreAntibacterial activity of CNSs against Staphylococcus aureus and Escherichia coli was estimated. Higher inhibition zone of 18 mm and 20 mm were observed against S. aureus and E.coli, respectively, at a concentration of 2 mg/ml of carbon nanosphere after 24 hrs of incubation at 37 ºC. In vitro cytotoxicity experiment was performed on two parasite strains of Leishmania donovani and Leishmania tropica by using MTT assay. L. donovani revealed more sensitiv to the CNSs than L. tropica. An intermediate level of cytotoxicity of 51.31 % was observed when 2.4 mg/ml of CNSs was incubated with L. donovani, while weak cytotoxicity of 37.20 % was shown when the
... Show MoreThe antimicrobial potency of the crude ethanolic extracts from different Iraqi plants were evaluated . Further more, total sesquiterpene lactones and phenolic compounds were isolated and their antimicrobial activity attempted. The results indicated that crude extracts have no activity except that of Callistemon lanceolatus. Also, the sesquiterpene lactones and phenolic compounds isolated from Callistemon lanceolatus were the most significant antimicrobial active constituents of the studied plants.
The purpose of this study is to determine the useful of Schiff bases derivatives containing (oxazepine, tetrazole) rings with biological activity which can be used as drug and antimicrobial, the present work is started from [Binary (2,5(4,'4-diaminophenyl) – 1,3,4 – oxadiazole]. A variety of Schiff bases and heterocyclic (oxazepine, tetrazole) have been synthesis, and confirm that structures by physical properties , FTIR , 1H-NMR, 13C-NMR, elemental analysis, [Microbial study against three type of bacteria (staphylococcus aurea and klebsiella pneumonia) and (Canadida albncans) fungi].All analyzation performed in center of consulatation University of Jordan.
Sulfamethoxazole (SMX) is the most significant antibiotic in the sulfonamide family. It was chosen as the representative of this category because of its widespread use. Starting with sulfamethoxazole, a new series of 2-Azetidinone (M1-M6) was synthesized, the structure of these new derivatives was confirmed using spectral methods, starting with the synthesis of Schiff’s bases by reflux of different aromatic benzaldehydes, separately, with Sulfamethoxazole in ethanol with few drops of acetic acid. The final compounds were obtained by ketene-imine synthesis of β-lactam using chloroacetyl chloride. The designed chemicals’ synthesis has been completed successfully. Physical parameters (melting points and Rf values), Fourier transfo
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