In the present study, five derivatives have been designed to be synthesized as possible mutual prodrugs for 5-Fluorouracil (5-FU) and non steroidal anti-inflammatory drugs (NSAIDs) to selectively deliver the drugs into the cancer cells. The synthesis of the target compounds were accomplished following multistep reaction procedures, the chemical reaction followed up and the purity of the products were checked by TLC. The structure of the final compounds and their intermediates were confirmed by their melting points, infrared spectroscopy and elemental microanalysis, the hydrolysis of compound III was studied using HPLC technique. According to the results mentioned above, compounds (I−V) can be good candidates as possible mutual prod
... Show MoreA series of coumarin derivatives linked to amino acid ester side chains were synthesized and evaluated of their antibacterial and antifungal activity. The coumarin derivatives was alkylated by the ethyl bromoacetate and then using potassium carbonate to get alkylated hymecromone. Conventional solution method for amide bond formation was used as a coupling method between the carboxy-protected amino acids with acetic acid side chain of coumarin derivatives. The DCC/ HOBt coupling reagents were used for peptide bond formation. The proposed analogues were successfully synthesized and their structural formulas were consistent with the proposed struct
... Show MoreThe development of new cephalosporins with improved activity against resistant microbes, such as, MRSA (methicillin resistant Staph. aureus), P. aeruginosa, is of high potential. Chemical synthesis of two new series of thiadiazole linked to cysteine (series 1) and cephalosporins containing thiadiazole linked to cysteine through disulfide bond (series 2) were achieved. The chemical structures of the synthesized compounds were confirmed using spectral (FT-IR, 1H-NMR) and elemental microanalysis. The incorporation of privileged chemical moieties, such as, thiadiazole, Schiff base, cysteine and sulfonamide, has been found to have great contribution to the antimicrobial activities. Compounds of series 1 (1
... Show MoreNewly 4-amino-1,2,4-triazole-3-thione ring 2 was formed at position six of 2-methylphenol from the reaction of 6-(5-thio1,3,4-oxadiazol-2-yl)-2-methylphenol 1 with hydrazine hydrochloride in the presence of anhydrase sodium acetate. Seven newly fused heterocyclic compounds were synthesized from compound 2. First fused heterocyclic was 6-(6-(3,5-di-tertbutyl-4-hydroxyphenyl)-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazol-3-yl)-2-methylphenol 3 synthesized from reaction compound 2 with 3,5-di-tert-butyl-4-hydroxybenzoic acid in POCl3. Reaction compound 2 with bromophencylbromide afford 6-(6-(4-bromophenyl)-5H-[1,2,4]triazolo[3,4-b][1,3,4]-thiadiazin-3-yl)-2-methylphenol 4. 6-(6-thio-1,7a-dihydro-[1,2,4] triazolo[3,4-b][1,3,4]-thiadiazol-3-yl)-2
... Show MoreIn this paper new methods were presented based on technique of differences which is the difference- based modified jackknifed generalized ridge regression estimator(DMJGR) and difference-based generalized jackknifed ridge regression estimator(DGJR), in estimating the parameters of linear part of the partially linear model. As for the nonlinear part represented by the nonparametric function, it was estimated using Nadaraya Watson smoother. The partially linear model was compared using these proposed methods with other estimators based on differencing technique through the MSE comparison criterion in simulation study.
In this paper, Bayes estimators of the parameter of Maxwell distribution have been derived along with maximum likelihood estimator. The non-informative priors; Jeffreys and the extension of Jeffreys prior information has been considered under two different loss functions, the squared error loss function and the modified squared error loss function for comparison purpose. A simulation study has been developed in order to gain an insight into the performance on small, moderate and large samples. The performance of these estimators has been explored numerically under different conditions. The efficiency for the estimators was compared according to the mean square error MSE. The results of comparison by MSE show that the efficiency of Bayes est
... Show MoreIn this paper, Bayes estimators of the parameter of Maxwell distribution have been derived along with maximum likelihood estimator. The non-informative priors; Jeffreys and the extension of Jeffreys prior information has been considered under two different loss functions, the squared error loss function and the modified squared error loss function for comparison purpose. A simulation study has been developed in order to gain an insight into the performance on small, moderate and large samples. The performance of these estimators has been explored numerically under different conditions. The efficiency for the estimators was compared according to the mean square error MSE. The results of comparison by MSE show that the efficiency of B
... Show MoreThe accumulation of construction and demolition waste is one of the major problems in modern construction. Hence, this research investigates the use of waste brick in concrete. Seven different concrete mixes were investigated in this study: a control concrete mix, three mixes with volumetric replacement (10, 20, and 30)% of natural aggregate with brick aggregate, and two mixes with the addition of nano brick powder at a percentage level of 5– 10% by weight of cementitious materials. And the last one was mixed with 10% nano brick and 10% coarse brick aggregate. The experimental results for the additive of nano brick powder showed an enhancement in mechanical properties (compressive,
This research involved synthesis of new β-Lactam derivative from Azo compound[4-amino-N-(pyrimidine-2-yl)-3-(pyrimidine-2-yldiazenyl) benzene sulfonamide] (S1) record previously by many steps. Starting conversion the free amino group in an azo comp. to chloro acetamide derivative(S2), then reacted it with urea to give the oxazole ring derivative (S3) that which containing free amino group. The condensation reaction between the amino group and P-bromobenzaldehyde to produce Shiff base (B14). Finally staudinger's cyclo addition reaction go run between the Shiff base derivative (B14) and chloro acetyl chloride in the presence of tri ethyl amine (Et3N) as Base catalyst and dioxane a
... Show MoreComparison is the most common and effective technique for human thinking: the human mind always judges something new based on its comparison with similar things that are already known. Therefore, literary comparisons are always clear and convincing. In our daily lives, we are constantly forced to compare different things in terms of quantity, quality, or other aspects. It is known that comparisons are used in literature in order for speech to be clear and effective, but when these comparisons are used in everyday speech, it is in order to convey the meaning directly and quickly, because many of these expressions used daily are comparisons. In our research, we discussed this comparison as a means of metaphor and expression in Russia
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