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951.
    
The phenylhydrazones 1a‐d condensed with ethyl cyanoacetate to yield pyridazinones 2a‐d that reacted with sulphur in presence of piperidine to yield the aminothienopyridazineones 3a,b that reacted with electron poor olefins and acetylenes to yield phthalazines 10‐12. The condensed aminothiophenes 3a,b reacted with dimethylformamide dimethylacetal to yield amidines 13a,b. Compounds 2a,b condensed with dimethylformamide dimethylacetal to yield the trans enamines 16a,b that cyclized readily into the pyridopyridazinones 17a,b on treatment with ammonium acetate in presence of acetic acid. Compounds 2a‐d reacted also with benzylidenemalononitrile to yield the phthalazinones 21a‐d. The reactions were conducted both by microwave heating and conventional heating. Better yields in much shorter reaction times were achieved by microwave heating.  相似文献   
952.
    
A number of new [(pyrazol‐4‐yl)methylene]hydrazono‐2,3‐dihydrothiazole derivatives, their sugar hydrazones and N‐glycosides were synthesized. Furthermore, N‐substituted oxygenated alkyl and hydroxyl derivatives and 1,3,4,‐oxadiazoline acyclic nucleoside analogs were prepared. The newly synthesized compounds were tested for their antimicrobial activities and showed moderate to high inhibition activities. J. Heterocyclic Chem., (2012).  相似文献   
953.
    
Thirty‐three species of mosquitoes have been reported from the Kingdom of Saudi Arabia. Several of these mosquitoes, Anopheles gambiae Giles s.l., Anopheles stephensi Liston, Culex pipiens Linnaeus, Culex quinquefasciatus Say, Culex tritaeniorhynchus Giles, Stegomyia aegypti (Linnaeus) and Aedimorphus vexans arabiensis (Patton) are known vectors of human and animal diseases. In this study, the cuticular hydrocarbon profiles of eight mosquito species using gas chromatography–mass spectrometry were analyzed. Wild collected fourth‐instar larvae were reared, and single, newly emerged, unfed adult females were used for the analysis. A total of 146–160 peaks were detected from the cuticular extracts by gas chromatography. Repeated analysis of variance (ANOVA) and Tukey HSD Post Hoc test was used to test for quantitative differences in relative hydrocarbon quantity. In addition, a linear regression model was applied using Enter method to determine the diagnostic peaks for the eight mosquito specimens. The ANOVA test indicated that relative peaks were significant (P < 0.05) when selected pairs of peaks were compared. Also, seven compounds showed qualitative differences among the five mosquito vectors tested. The classes of constituents present were n‐alkanes, monomethylalkanes, dimethylalkanes, trimethylalkanes, alkenes, branched aromatic hydrocarbons, aldehydes and esters. These compounds have a carbon chain length ranging from 8 to 18 carbons. The most abundant compound in all adult mosquito specimens was n‐hexylacrylate [retention time (RT) 6.73 min], which was not detected in Cx. pipiens. In Cx. pipiens, the most abundant peak was benzaldehyde (RT 2.98 min). Gas chromatography–mass spectrometry is a suitable method to identify adult mosquitoes, especially from focal areas of public health concern such as Jazan Province, Saudi Arabia. This method allows a wide range of adult collected material to be identified with high accuracy. Copyright © 2013 John Wiley & Sons, Ltd.  相似文献   
954.
    
Diethyl azodicarboxylate and 3,4,5,6‐tetrachloro‐1,2‐benzoquinone react with cyclopentano‐ and cycloheptano‐fused thienopyrimidines to form the oxidative dimer of the starting material via S—S bond formation. Reaction of two equivalents of 2,2′‐(cyclohexa‐2′,5′‐diene‐1,4‐diylidene)dimalononitrile with thienopyrimidines afforded 3‐(4′,4′‐dicyanomethylene‐cycloalka[a]‐2,5‐dienyl)‐4‐oxo‐6,7,8,9‐tetrahydro‐5H‐cyclo‐hepta[4,5]‐[1,3]thiazolo[3,2‐a]‐thieno[2,3‐d]pyrimidin‐2‐ylidene‐2‐dicarbonitriles. The thioenopyrimidines react with 2‐[1,3‐dioxo‐1H‐inden‐2(3H)‐ylidene]malononitrile to produce 1,3,5′‐trioxo‐1,3,3′,5′‐tetrahydrospiro‐(indene‐2,2′‐thiazolo[2,3‐b]‐cycloalkyl[b]‐thieno[2,3‐d]pyrimidine)‐3′‐carbonitriles. However, the reaction of thienopyrimidines with 2,3‐dicyano‐1,4‐naphthoquinone proceeded to afford the fused cycloalkyl‐thieno form of naphtho[1,3]thiazolo[3,2‐a]thieno[2,3‐d]pyrimidine‐6.7,12‐triones. Reaction of 2‐hydrazino‐5,6,7,8‐tetrahydrobenzo[b]thieno[2,3‐d]pyrimidine‐4(1H)‐one with dimethyl acetylenedicarboxylate and ethyl propiolate, respectively, afforded cyclohexano‐fused (Z)‐dimethyl 2[(E)‐4‐oxo‐3,4‐dihydrothieno[2,3‐d]pyrimidine‐2(1H)‐ylidene)hydrazono]succinate and thieno‐pyrimidinotriazine. Both oxidative dimers of thienopyrimidines showed high inhibition of Hep‐G2 cell growth compared with the growth of untreated control cells. Moreover, the cycloheptano‐fused thiazinothienopyrimidine indicates a promising specific antitumor agent against Hep‐G2 cells because its IC50 is < 20 μM.  相似文献   
955.
    
A capillary zone electrophoretic method has been developed and validated for the determination of the impurity quinocide (QC) in the antimalarial drug primaquine (PQ). Different buffer additives such as native cyclodextrins and crown ethers were evaluated. Promising results were obtained when either β‐cyclodextrin (β‐CD) or 18‐crown‐6 ether (18C6) were used. Their separation conditions such as type of buffer and its pH, buffer additive concentration, applied voltage capillary temperature and injection time were optimized. The use of 18C6 offers slight advantages over β‐CD such as faster elution times and improved resolution. Nevertheless, migration times of less than 5 min and resolution factors (Rs) in the range of 2–4 were obtained when both additives were used. The method was validated with respect to selectivity, linearity, limits of detection and quantitation, analytical precision (intra‐ and inter‐day variability) and repeatability. Concentrations of 2.12 and 2.71% (w/w) of QC were found in pharmaceutical preparations of PQ from two different manufacturers. A possible mechanism for the successful separation of the isomers is also discussed. Copyright © 2008 John Wiley & Sons, Ltd.  相似文献   
956.
    
2‐(Arylidene)cyanomethylbenzoxazoles have been prepared in water from benzoxazole‐2‐ylacetonitriles. Using multi‐component reactions, a variety of heterocycles containing benzoxazole and nitrile functionality has been prepared. J. Heterocyclic Chem., (2011).  相似文献   
957.
    
Thiation of 1 by LR gave the corresponding 3,5‐dithioxo derivative 2 and the trimer 3 . Methylation of 1 afforded the S‐methyl derivative 4 . Compound 1 was fused with 6‐bromo‐2‐phenyl‐benzo[1,3‐d]oxazin‐4‐one ( 5 ) and gave 6 . Condensation of 1 with some acid derivatives 7a , 7b , 7c , 7d and/or 8a , 8b , 8c yielded thiadiazolo‐triazine derivatives 9a , 9b , 9c , 9d and 10a , 10b , 10c . Compounds 9a , 9c and 10c were hydrolyzed to furnish 11a , 11b , 11c Acetylation of 14 afforded mono‐ and diacetyl‐derivatives 15 and 16 . Benzoylation of 14 afforded mono‐ and dibezoyl‐derivatives 17 and 18 . 14 with some aromatic aldehydes yielded 9a , 9b , 9c . Reacting 14 with phenyl (iso‐ and/or isothio‐) cyanate gave the urea derivatives 20a , 20b . Thiation of 14 with P4S10 furnished 21 . The newly synthesized compounds were tested as antimicrobial agents. J. Heterocyclic Chem., (2011)  相似文献   
958.
    
We demonstrate a facile methodology for the production of metallic electrocatalytic microdomain ensembles for a range of analytical sensing challenges. A commercially available off‐the‐shelf cosmetic product can change the voltammetric characteristics of a metallic macro‐electrode created electrolytically into that of a random ensemble of metallic microelectrode domains. Proof‐of‐concept is shown for three examples: a palladium ensemble for hydrazine sensing, a gold ensemble for arsenic(III) detection via anodic stripping voltammetry and platinum ensembles for the direct oxidation of arsenic(III). Last we demonstrate that the fabrication of metallic microdomains can be simplified by sputter coating screen printed electrochemical sensing platforms which are beneficially constructed using this cosmetic methodology. Given the facile fabrication and low cost of the underlying electrode substrate and the cosmetic modifier, the widespread implementation of this novel fabrication methodology is expected.  相似文献   
959.
    
Gold ensembles for the trace level sensing of arsenic(III) in the presence of copper(II) are reported. The gold ensembles are fabricated using citrate capped gold nanoparticles which are chemically synthesised in an aqueous solution with an aliquot of this simply cast onto an economical and disposable screen printed electrode. After drying at room temperature, the gold ensembles are ready for use. The gold ensembles are explored towards the sensing of arsenic(III) in the presence of copper(II) using anodic stripping voltammetry where the corresponding stripping peaks are well resolved and using this protocol it is possible to readily detect 3 µg L?1 (3 ppb) with a detection limit of 0.4 µg L?1 (0.4 ppb). Proof‐of‐concept is also shown for the sensing of arsenic(III) in a canal water sample. Given the low cost of the sensor and ease of fabrication, the gold ensembles hold promise for the sensing of arsenic(III) in water samples where copper(II) may be present.  相似文献   
960.
    
Pd(DME)Cl2 complex was synthesized and characterized, where DME is 2‐{[2‐(dimethylamino)ethyl]‐methylamino}ethanol. Stoichiometry and stability constants of the complexes formed between various biologically relevant ligands (amino acids, peptides, DNA constituents, and dicarboxylic acids) and [Pd(DME)(H2O)2]2+ are investigated at 25°C and at constant 0.1 M ionic strength. The effect of dielectric constant of the medium on the stability constant of Pd(DME)‐CBDCA complex, where CBDCA is cyclobutanedicarboxylate, is also reported. The concentration distribution diagrams of the various species formed are evaluated. The kinetics of base hydrolysis of amino acid esters coordinated to Pd(DME)2+ complex is investigated. The effect of the temperature on the kinetics of base hydrolysis of glycine methyl ester complex is studied. © 2010 Wiley Periodicals, Inc. Int J Chem Kinet 42: 608–618, 2010  相似文献   
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