Non-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 sulphonamide to form final compounds ( III a-b) .The structures of these compounds were identified and characterized using (TLC), infrared spectroscopy (FT-IR), 1H NMR data and microanalysis (CHN).Pharmacological study as anti-inflammatory activities for the final compounds were studied in rats by induced edema type of inflammation. Moreover, the results of a docking study of compounds III a-b into the COX-2 binding site revealed that its mechanism was possibly similar to that of naproxen, a COX-2 inhibitor. The effect of them on COX-2 antibody was showed it could significantly inhibit COX-2 activity.
In this paper, a description of a design for new DES block cipher, namely DES64X and DES128X. The goals of this design, a part of its security level, are large implementation flexibility on various operating systems as well as high performances. The high level structure is based on the principle of DES and Feistel schema, and proposes the design of an efficient key-schedule algorithm which will output pseudorandomsequences of subkeys. The main goal is to reach the highest possible flexibility, in terms of round numbers, key size, and block size. A comparison of the proposed systems on 32-bit, 64-bit operating system, using 32-bit and 64-bit Java Virtual Machine (JVM), showed that the latter has much better performance than the former.
... Show MoreOne of the most important , compound which have active hydrogen is the compound possessing (thiol group) Biphenyl-4,4-dithiol is agood example utilized in a wide field for preparation mannich bases , avariety of new acetylenic mannich bases have been Synthesized and all proposed structure were Supported by FTIR , 1H – NMR, 13C-NMR , Elemental analysis and microbial study .
The formation and structural investigation of three new Mannich bases are reported. The synthesis of these compounds was accomplished via a multicomponent one-pot reaction using CaCl2 as a catalyst. The reaction of the benzaldehyde, m-bromoaniline and cyclohexanone or 4-methylcyclohexanone resulted in the formation of L1 and L3, respectively. The synthesis of L2 was achieved by mixing benzaldehyde, o-bromoaniline and cyclohexanone. The isolated compounds were characterised using a range of analytical and spectroscopic techniques. These include; NMR (1H and 13C-NMR), ESMS, FTIR, electronic spectroscopy, microanalyses and melting points. The NMR data for L1 and L2 indicated the presence of one isomer in solutions, on the NMR time scale. How
... Show MoreNew N2O2 donor kind Schiff basehas been destined and structured by reaction Ampyrone with O-hydroxyacetophenone and Anthranilic acid. The metal complexes of the Schiff base with Mn(II), Hg(II), Ni(II), Cu(II), and Co(II) metal ions were designed and characterized by magnetic susceptibility, elemental analyses, molar conduction, IR, and 1H NMR,UV-Vis spectral metrics.The UV-Vis. and magnetic susceptibility data of the complexes suggest a square-planar, tetrahedraland octahedral geometries around the central metal ions. All elaborations were accomplished after determination the optimum molar concentration and pH which followed law of Lambert-Beer's in the researches pH scopes. The composition of these complexes were conclude dapprobating to t
... Show MoreCoumarin is a natural substance isolated from different plants. It belonges to a group of benzobyrones which consists of a benzene ring joined to a pyrone nucleus. In the present research, a new series of coumarin derivatives were formed. Compound (1) (7-hydroxy-4-methyl Coumarin) was converted into 4-methylquinolin-2(H) derivative (2) by reaction with acetamide, and then reaction of (2) with thiosemicarbazide in ethanol leads to the synthesize of hydrazincarbothioamide derivative (3).The reaction of (3) with ethylchloroacetate in presence of sodium acetate leads to closure ring to get [(1-(5-oxo-2-thioxoimidazolidin-1-ylimino) ethyl)]quinolin-2(1H)-one (4). Mannich bases were prepared through the reaction of (4) with primary
... Show MoreBackground: Isoxazoles are an important class of five-membered unsaturated heterocyclic compounds. They show several applications in diverse areas such as pharmaceuticals, agrochemistry and industry. Isoxazoles are also found in natural sources showing insecticidal, plant growth regulation and pigment functions. Current study was conducted for synthesis of twenty five new Isoxazole derivatives and to evaluate the in vitro antibacterial activities of these derivatives. Methods: Benzaldoxime and their substituted [I] ae were prepared via addition-elimination reactions between aromatic aldehyde and hydroxylamine hydrochloride. In a second step, para-or meta-substituted benzaldoximes [I] ae were reacted with N-chlorosucceinimide in DMF to yield
... Show MoreThis paper considers and proposes new estimators that depend on the sample and on prior information in the case that they either are equally or are not equally important in the model. The prior information is described as linear stochastic restrictions. We study the properties and the performances of these estimators compared to other common estimators using the mean squared error as a criterion for the goodness of fit. A numerical example and a simulation study are proposed to explain the performance of the estimators.
Abstract As a part of our ongoing project on the design and synthesis of new 4-thiazolidinone derivatives with antimicrobial activity, four new 4-thiazolidinone derivatives carrying bromo, nitro, methyl, and chloro groups on the benzene ring were synthesized by starting with the 7-amino-4-methylcoumarin moiety, linking coumarin with various phenyl isothiocynate to form the thiourea group, and then cyclizing the derivatives, characterized by IR and 1HNMR, and assayed in vitro for their antimicrobial activity against Gram positive and Gram negative bacteria and fungi. Overall, 2-(4-methyl-2-oxo-2H-chromen-3-yl)-3-(4-nitrophenyl) thiazolidin-4-one to be the most powerful individuals in the series. Based on the observed data, it can be sta
... Show MoreMotifs template is the input for many bioinformatics systems such codons finding, transcription, transaction, sequential pattern miner, and bioinformatics databases analysis. The size of motifs arranged from one base up to several Mega bases, therefore, the typing errors increase according to the size of motifs. In addition, when the structures motifs are submitted to bioinformatics systems, the specifications of motifs components are required, i.e. the simple motifs, gaps, and the lower bound and upper bound of each gap. The motifs can be of DNA, RNA, or Protein. In this research, a motif parser and visualization module is designed depending on a proposed a context free grammar, CFG, and colors human recognition system. GFC describes the m
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