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Full-Text Articles in Chemistry

Mono-N-Acyl-2,6-Diaminopimelic Acid Derivatives: Analysis By Electromigration And Spectroscopic Methods And Examination Of Enzyme Inhibitory Activity, Jan Hlaváček, Miloslava Vítovcová, Petra Sázelová, Jan Pícha, Václav Vaněk, Miloš Buděšínský, Jiří Jiráček, Danuta Gillner, Richard Holz, Ivan Mikšík, Václav Kašička Mar 2015

Mono-N-Acyl-2,6-Diaminopimelic Acid Derivatives: Analysis By Electromigration And Spectroscopic Methods And Examination Of Enzyme Inhibitory Activity, Jan Hlaváček, Miloslava Vítovcová, Petra Sázelová, Jan Pícha, Václav Vaněk, Miloš Buděšínský, Jiří Jiráček, Danuta Gillner, Richard Holz, Ivan Mikšík, Václav Kašička

Richard C. Holz

Thirteen mono-N-acyl derivatives of 2,6-diaminopimelic acid (DAP)—new potential inhibitors of the dapE-encoded N-succinyl-l,l-diaminopimelic acid desuccinylase (DapE; EC 3.5.1.18)—were analyzed and characterized by infrared (IR) and nuclear magnetic resonance (NMR) spectroscopies and two capillary electromigration methods: capillary zone electrophoresis (CZE) and micellar electrokinetic chromatography (MEKC). Structural features of DAP derivatives were characterized by IR and NMR spectroscopies, whereas CZE and MEKC were applied to evaluate their purity and to investigate their electromigration properties. Effective electrophoretic mobilities of these compounds were determined by CZE in acidic and alkaline background electrolytes (BGEs) and by MEKC in acidic and alkaline BGEs containing a pseudostationary …


Synthesis Of Novel 1,2,4-Triazoles And Triazolo-Thiadiazines As Anticancer Agents, Thoraya Abd El-Reheem Farghaly, Magda Ahmad Abdallah, Huda Kamel Mmahmoud Jan 2015

Synthesis Of Novel 1,2,4-Triazoles And Triazolo-Thiadiazines As Anticancer Agents, Thoraya Abd El-Reheem Farghaly, Magda Ahmad Abdallah, Huda Kamel Mmahmoud

Turkish Journal of Chemistry

A new series of 7-arylazo-5$H$-3-(trifluoromethyl)-6-methyl-1,2,4-triazolo-[3,4-$b$]-1,3,4-thiadiazines was prepared by reaction of 4-amino-3-trifluoromethyl-5-mercapto-1,2,4-triazoles with $N$-aryl-2-oxo-propane hydrazonoyl chloride in dioxane under reflux in the presence of triethylamine. Furthermore, Schiff bases of 4-amino-5-mercapto-1,2,4-triazole derivatives were reacted with a variety of hydrazonoyl chlorides and gave the respective hydrazonothioates. In addition, the novel \textit{bis}-(1,2,4-triazole-3-thione) was reacted with the appropriate hydrazonoyl chloride in dioxane under reflux in the presence of triethylamine to give the corresponding \textit{bis}-(1,2,4-triazolethiohydrazonoate). The structures of the new compounds were established based on elemental and spectral data. The mechanism of the studied reaction was also discussed. Moreover, some of the new products were screened …


Microwave-Assisted Synthesis Of Novel 8-Chloro-[1,2,4]Triazolo[4,3-$A$]Pyridine Derivatives, Linjiong Zhang, Mingyan Yang, Beizhen Hu, Zhaohui Sun, Xinghai Liu, Jianquan Weng, Chengxia Tan Jan 2015

Microwave-Assisted Synthesis Of Novel 8-Chloro-[1,2,4]Triazolo[4,3-$A$]Pyridine Derivatives, Linjiong Zhang, Mingyan Yang, Beizhen Hu, Zhaohui Sun, Xinghai Liu, Jianquan Weng, Chengxia Tan

Turkish Journal of Chemistry

A series of novel 1,2,4-triazolo[4,3-$a$]pyridine derivatives were synthesized from 2,3-dichloropyridine and hydrazine hydrate as starting materials by multistep reactions under microwave assistance, and their structures were characterized by $^{1}$H NMR, MS, and elemental analysis. This method provides several advantages such as high yields, facile work-up, and environmental friendliness.


Reactivity Of The 2-Aryl-6,8-Dibromo-2,3-Dihydroquinolin-4(1$H)$-Ones In A Palladium Catalyzed Sonogashira Cross-Coupling Reaction, Malose Jack Mphahlele, Felix Adetunji Oyeyiola Jan 2015

Reactivity Of The 2-Aryl-6,8-Dibromo-2,3-Dihydroquinolin-4(1$H)$-Ones In A Palladium Catalyzed Sonogashira Cross-Coupling Reaction, Malose Jack Mphahlele, Felix Adetunji Oyeyiola

Turkish Journal of Chemistry

Pd/C-PPh$_{3}$--CuI catalyzed Sonogashira cross-coupling of the 2-aryl-6,8-dibromo-2,3-dihydroquinolin-4(1$H)$-ones with phenyl acetylene or 3-butyn-1-ol afforded the corresponding 8-alkynylated quinolin-4(1$H)$-one derivatives, exclusively. Double carbo-substitution to afford the 6,8-dialkynyl derivatives was observed when PdCl$_{2}$(PPh$_{3})_{2}$ was used as Pd(0) source. The monoalkynylated derivatives were, in turn, subjected to PdCl$_{2}$ in acetonitrile under reflux to afford either the corresponding 2,4-diaryl-8-bromopyrrolo[3,2,1-\textit{ij}]quinolinones or the 8-(4-hydroxybutanoyl)-substituted quinolinone derivatives, exclusively. Suzuki--Miyaura cross-coupling of the 2-aryl-6-bromo-8-(alkynyl)quinolin-4-ones afforded the 2,4,8-trisubstituted pyrrolo[3,2,1-\textit{ij}]quinolin-6-ones.