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MM. J. Duflos D. Letouz G. Queguiner P. Pastour 《Journal of heterocyclic chemistry》1973,10(6):1083-1084
This communication describes the synthesis of l-methyl-2,3-diformylpyrrole. This new compound is used to prepare a new heterocycle, l-methylcyclohepta[b]pyrrol-6-one and thus allows a new synthesis of l-methylpyrrolo[2,3-d]pyridazine. 相似文献
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Z. H. Ismail M. M. Ghorab E. M. A. Mohamed H. M. Aly M. S. A. El-Gaby 《Phosphorus, sulfur, and silicon and the related elements》2013,188(10):2541-2554
Some novel thiourea,1,2,4-triazole, quinazoline, thieno[2,3-d]pyrimi-dine, and thiazolidine derivatives were synthesized to evaluate their antitumor activity. Compound (3f) is nearly as active as reference drug, (Doxorubicin) as positive control. 相似文献
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M. M. Ghorab N. E. Amin M. S. A. El Gaby N. M. H. Taha M. A. Shehab I. M. I. Faker 《Phosphorus, sulfur, and silicon and the related elements》2013,188(12):2918-2928
The key intermediate diisothiocyanate 2 was allowed to react with 5-amino-3-methyl-pyrazole-4-carbonitrile 3, ethyl 5-amino-1-phenyl-pyrazole-4-carboxylate 6, 2-amino-tetrahydrobenzo[b]thiophene-3-car-bonitrile 9, ethyl-2-amino-tetra-hydrobenzo[b]thiophene-3-carboxylate 12, and/or 1,2,4-triazole 15 to give the corresponding biscompounds 4, 5, 7, 8, 10, 11, 13, 14, and 16, respectively. The structure of the synthesized compounds was elucidated by elemental analyses and spectral data. Some of the prepared compounds were tested for their antimicrobial and antitumor activities. 相似文献
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Kareem AbuBakr Soliman Howida Kamal Ibrahim Mahmoud Mohamed Ghorab 《Journal of Dispersion Science and Technology》2013,34(8):1127-1133
Risperidone is an atypical antipsychotic drug used to treat schizophrenia. This study aims to formulate risperidone as effervescent tablets to improve patient compliance. Different nanoemulsion combinations were loaded with risperidone to improve its poor water solubility then adsorbed on Aeroperl. The formula showing highest drug dissolution was formulated as effervescent tablets. Factorial design was applied for different tablet formulation variables and the prepared formulae were tested for different criteria in comparison with their corresponding formulae containing drug without nanoemulsion formulation. Statistical analysis was used to determine the most desirable tablet formula considering its Carr index, effervescence time, and drug release. 相似文献
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H. O. Ammar M. Ghorab D. M. Mostafa T. S. Makram R. M. Ali 《Journal of inclusion phenomena and macrocyclic chemistry》2013,77(1-4):121-134
Etodolac, being a practically insoluble candidate, exhibits certain toxic effects and a limited bioavailability. Upon chronic use, it causes gastro-intestinal injury and increases the risk of ulcer complications. The approach of this study was to improve the physicochemical properties of the drug utilizing complexation phenomenon with β-, methyl-β- and hydroxypropyl-β-cyclodextrins, which may enhance the aqueous solubility and dissolution rate of etodolac, in an effort to increase oral bioavailability. In certain instances, this approach can be used to increase drug solubility, improve organoleptic properties and maximize the gastrointestinal tolerance by reducing drug irritation after oral administration. Differential UV measurements as well as continuous variation plots revealed the formation of equimolar complex with hydroxypropyl-β-cyclodextrin and 1:2 complexes with β-cyclodextrin and its methyl derivative. Differential scanning calorimetry (DSC), X-ray and FT-IR measurements were applied to prove inclusion complex formation and characterize the complexes. These results lend support to the idea that solubilization of etodolac is mainly related to inclusion complex formation and to a lesser extent to cyclodextrin aggregates. Understanding the factors that influence the performance of etodolac, will allow us to state that molecular encapsulation of the drug and other modifications with appropriate hydroxylation or methylation of parent β-cyclodextrin is able to overcome its problems and facilitate safe and efficient delivery of the drug. 相似文献
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Mostafa M. Ghorab Mansour S. Al‐Said Ebaa M. El‐Hossary 《Journal of heterocyclic chemistry》2011,48(3):563-571
Sulfonamide‐bearing compounds posses many types of biological activities and have been recently reported to show substantial antitumor activity in vitro and/or in vivo. There are a variety of mechanisms for the anticancer activity, and the most prominent mechanism is the inhibition of carbonic anhydrase isozymes. This work reports the synthesis of some new quinoline, pyrimido[4,5‐b]quinoline and 3,1‐oxazinoquinoline derivatives bearing a sulfonamide moiety. All the newly synthesized compounds were evaluated for their in vitro anticancer activity against Ehrlich ascites carcinoma cells. Compounds 10 , 13 , and 26 were the most active compounds with IC50 values of 6.1 μM, 6.8 μM, and 6.4 μM, respectively, and exhibited better activities than the reference drug doxorubicin (IC50 = 68.1 μM). J. Heterocyclic Chem., 2011. 相似文献
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MM. P. Duballet A. Godard G. Queguiner P. Pastour 《Journal of heterocyclic chemistry》1973,10(6):1079-1080
This article describes the synthesis of a new heterocycle, pyrido[2,3,f]phtalazine and three new diformylquinolincs. 相似文献