The work includes synthesis and characterization of some new heterocyclic compounds, as flow: The compound (3) (5-(4-chlorophenyl) -2-hydrazinyl-1,3,4-oxadiazole was synthesized by using two methods; the first method includes the direct reaction between hydrazine hydrate 80% and 5-(4-chlorophenyl)-2- (ethylthio) 1,3,4-oxadiazole (1), the second method involves converting 5-(4-chlorophenyl)-1,3,4-oxadiazol-2-amine (2) to diazonium salt then reducing this salt to compound (3) by stannous chloride. Compound (3) was used as starting material for synthesizing several fused heterocyclic compounds. The compound 6-(4-chlorophenyl)[1,2.4] triazolo [3,4,b][1,3,4] oxadiazole-3-(2H) thione (compound 4) was synthesized from the reaction of compound (3) with carbon disulfide in presence of potassium hydroxide. Compound 6-(4-chlorophenyl)-[1,2,4] triazolo [3,4-b][1,3,4] oxadiazole-3-amine (5) was synthesized from treatment of compound (3) with cyanogen bromide at room temperature in the presence of sodium hydrogen carbonate. Direct reaction between acetic acid and compound (3) in POCl3 affords 6-(4-chlorophenyl)-3-methyl-[1,2,4] triazolo [3,4,b][1,3,4] oxadiazole (compound 6). Five new fused rings derivatives (12-16) [6-(4-chlorophenyl)-3-(aryl)-[1,2,4] triazolo[3,4-b][1,3,4]oxadiazol] were synthesized by two steps. The first step was synthesized by corresponding Schiff bases (7-11) from reaction compound (3) with five aryl aldehyde. These Schiff bases were used as substrate to synthesize compounds (12-16) by treating these compounds with bromine in glacial acetic acid in dry sodium acetate.The synthesized compounds were characterized by FTIR,H-NMR,C-NMR and CHNS analysis.
In this study new derivatives of Schiff bases 5-8, 1, 3-oxazepine 9-16 and tetrazoles 17-19 have been synthesized from the new starting material 1 which has synthesized the reaction of one mole of dichloro acetic acid and two moles of thiophenol, the esters 2-3 were synthesized from the reaction of compound 1 with methanol or ethanol respectively in the presence of H2SO4 as catalyst then 2, 2-dithiophenylaceto Hydrazide 4 were synthesized from the reaction of 2 or 3 with hydrazine hydrate 80%, Schiff bases 5-8 were synthesized from the reaction of 4 with appropriate aldehyde or ketone. Treatment of Schiff bases with maleic and phathalic anhydride in dry benzene to give 1, 3-oxazepen derivatives 9-16 and with sodium azide in tetrahydrofuran
... Show More5-Fluorouracil is one of the commonly used chemotherapy drugs in anticancer therapy; unfortunately treatment with 5-FU by solely has many drawbacks low lipophilicity, low permeability, low molecular weight, and its relatively poor plasma protein binding; also a brief half-life therefore frequent administration is required to maintain the optimal therapeutic plasma level which in addition to its poor selectivity, drug resistance and limited penetration to cancer cells; leads to increased incidence of side-effects to healthy cells/tissues and low response rates. In order to minimize these drawbacks; 5-FU was chemically conjugated with pyrrolidine dithiocarbamate (PDTC) in a mutual prodrug moiety (S-(9H-purin-6-yl) 3-(
... 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 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 MoreThree of imide intermediate products were synthesized by reacting of phthalic anhydride with glycine (2a), and tetrachloro phthalic anhydride with glycine , (S)-2-[(tert-Butoxycarbonyl)amino]-3-aminopropionic acid ( 2b,c) respectively in dry toluene with azeotropic removal of water using Dean- stark apparatus then carboxyl functional group activated by refluxing with thionyl chloride, the resulted acid chloride (3a-c) were reacted with different amine (5-flourouracil, 4-chloroaniline, 4-bromoaniline, 2-amino thiazole, and pyrrolidine) (4a-e) , the resulted products consider as
... Show MoreIbuprofen is one of the most important members of NSAIDs, named aryl propionic acid derivative. Isatin (1H-indole-2,3-dione) is an important molecule of heterocyclic compounds that have many biological activities. This work illustrates the synthesis of new ibuprofen-isatin derivatives by connecting ibuprofen hydrazide with different isatin derivatives by a condensation reaction, followed by characterization by fourier-transform infrared spectroscopy (FTIR) and proton nuclear magnetic resonance (1H-NMR) spectroscopy. The anti-inflammatory activity was evaluated by using the egg-white induce edema method for all the synthesized compounds (5-8), the compounds 5 and 6 showed better anti-inflammatory activity than ibuprofen as a standard compoun
... Show MoreIbuprofen is one of the most important members of NSAIDs, named aryl propionic acid derivative. Isatin (1H-indole-2,3-dione) is an important molecule of heterocyclic compounds that have many biological activities. This work illustrates the synthesis of new ibuprofen-isatin derivatives by connecting ibuprofen hydrazide with different isatin derivatives by a condensation reaction, followed by characterization by fourier-transform infrared spectroscopy (FTIR) and proton nuclear magnetic resonance (1H-NMR) spectroscopy. The anti-inflammatory activity was evaluated by using the egg-white induce edema method for all the synthesized compounds (5-8), the compounds 5 and 6 showed better anti-inflammatory activity than ibuprofen as a standard
... Show MoreCertain cyclic amine derivatives of metronidazole via acetate spacer were prepared. Cyclic amines used are piperidine and piperazine to improve the physicochemical properties and reduce some of metronidazole side effects. This is believed to be done by modification of its structural features to get prodrugs with improved properties over that of metronidazole. The present work includes esterification of metronidazole with choroacetic acid, N-alkylation of the cyclic amines by the halogenated ester and characterization of their structures by spectral(UV and IR) and elemental(CHN)analysis.The melting points, degree of solubilities and partition coefficients were also determined. Both metronid
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