Open Access. Powered by Scholars. Published by Universities.®
Physical Sciences and Mathematics Commons™
Open Access. Powered by Scholars. Published by Universities.®
- Institution
- Publication
- Publication Type
Articles 1 - 9 of 9
Full-Text Articles in Physical Sciences and Mathematics
Spiroadamantyl 1,2,4-Trioxolane, 1,2,4-Trioxane, And 1,2,4-Trioxepane Pairs: Relationship Between Peroxide Bond Iron(Ii) Reactivity, Heme Alkylation Efficiency, And Antimalarial Activity, Xiaofang Wang, Darren J. Creek, Charles E. Schiaffo, Yuxiang Dong, Jacques Chollet, Christian Scheurer, Segio Wittlin, Susan A. Charman, Patrick Dussault, James K. Wood, Jonathan L. Vennerstrom
Spiroadamantyl 1,2,4-Trioxolane, 1,2,4-Trioxane, And 1,2,4-Trioxepane Pairs: Relationship Between Peroxide Bond Iron(Ii) Reactivity, Heme Alkylation Efficiency, And Antimalarial Activity, Xiaofang Wang, Darren J. Creek, Charles E. Schiaffo, Yuxiang Dong, Jacques Chollet, Christian Scheurer, Segio Wittlin, Susan A. Charman, Patrick Dussault, James K. Wood, Jonathan L. Vennerstrom
Patrick Dussault Publications
These data suggest that iron(II) reactivity for a set of homologous spiroadamantyl 1,2,4-trioxolane, 1,2,4-trioxane, and 1,2,4-trioxepane peroxide heterocycles is a necessary, but insufficient, property of animalarial peroxides. Heme alkylation efficiency appears to give a more accurate prediction of antimalarial activity than FeSO4-mediated reaction rates, suggesting that antimalarial activity is not merely dependent on peroxide bond cleavage, but also on the ability of reactive intermediates to alkylate heme or other proximal targets.
Spiroadamantyl 1,2,4-Trioxolane, 1,2,4-Trioxane, And 1,2,4-Trioxepane Pairs: Relationship Between Peroxide Bond Iron(Ii) Reactivity, Heme Alkylation Efficiency, And Antimalarial Activity, Xiaofang Wang, Darren J. Creek, Yuxiang Dong, Jacques Chollet, Christian Scheurer, Sergio Wittlin, Susan A. Charman, Patrick H. Dussault, James K. Wood, Jonathan L. Vennerstrom
Spiroadamantyl 1,2,4-Trioxolane, 1,2,4-Trioxane, And 1,2,4-Trioxepane Pairs: Relationship Between Peroxide Bond Iron(Ii) Reactivity, Heme Alkylation Efficiency, And Antimalarial Activity, Xiaofang Wang, Darren J. Creek, Yuxiang Dong, Jacques Chollet, Christian Scheurer, Sergio Wittlin, Susan A. Charman, Patrick H. Dussault, James K. Wood, Jonathan L. Vennerstrom
Chemistry Faculty Publications
These data suggest that iron(II) reactivity for a set of homologous spiroadamantyl 1,2,4-trioxolane, 1,2,4-trioxane, and 1,2,4-trioxepane peroxide heterocycles is a necessary, but insufficient, property of animalarial peroxides. Heme alkylation efficiency appears to give a more accurate prediction of antimalarial activity than FeSO4-mediated reaction rates, suggesting that antimalarial activity is not merely dependent on peroxide bond cleavage, but also on the ability of reactive intermediates to alkylate heme or other proximal targets.
Asymmetric Synthesis Of 1,2-Dioxanes: Approaches To The Peroxyplakoric Acids, Chunping Xu, Chris Schwartz, Joseph Raible, Patrick Dussault
Asymmetric Synthesis Of 1,2-Dioxanes: Approaches To The Peroxyplakoric Acids, Chunping Xu, Chris Schwartz, Joseph Raible, Patrick Dussault
Patrick Dussault Publications
The stereospecific intramolecular alkylation of a hydroperoxyacetal provides the basis for the first asymmetric synthesis of the dioxane propionate core of the peroxyplakorates. Chemoselective hydrometallation of an alkyne in the presence of a peroxide is used to introduce a synthon for the polyunsaturated side chains of the peroxyplakorates. The route suggests a general solution for the 1,2-dioxane unit in many peroxide natural products.
Design, Synthesis, And Characterization Of Novel Hydrophilic Fluorene-Based Derivatives For Bioimaging Applications, Dao Nguyen
Electronic Theses and Dissertations
In this work, hydrophilic fluorene-based derivatives that contain ethylene oxide substituents, have been synthesized and characterized for potential use as new fluorophores for bioimaging applications and for fluorescence sensing of heavy metals. Symmetrical and unsymmetrical fluorene derivatives based on structural types of acceptor-pi-acceptor, acceptor-pi-donor, and donor-pi-donor were characterized by TGA, UV-vis absorption, fluorescence emission, lifetime, anisotropy, and two-photon absorption (2PA) cross section. They were found to possess high thermal stability, high photostability, high fluorescence quantum yields, and generally large two-photon absorption cross sections, making them quite suitable for new probes in single-photon absorption and two-photon absorption fluorescence microscopy imaging. Novel …
A Convenient Synthesis Of 2-Azido And 2-Thiocyanato-2,3-Unsaturated Cyclic Ketones, Mesut Boz, Ömer Zai̇m, Hi̇lal Esen
A Convenient Synthesis Of 2-Azido And 2-Thiocyanato-2,3-Unsaturated Cyclic Ketones, Mesut Boz, Ömer Zai̇m, Hi̇lal Esen
Turkish Journal of Chemistry
2-Azido and 2-thiocyanato-2,3-unsaturated ketones were synthesized by utilizing functionalization of 5- or 6-membered cycloalkane-1,2-diones, namely diosphenols, with dimethylthiocarbomoyl chloride, which activates the system towards reaction with nucleophiles in acidic conditions. Replacement of the enolic oxygen of the diosphenols with azide and thiocyanate may be achieved by treating their dimethylthiocarbamates with sodium azide or potassium thiocyanate in boiling acetonitrile/acetic acid.
An Efficient One Pot Synthesis Of 1,4-Dihydropyridines Using Alumina Sulfuric Acid (Asa) Catalyst, Mustafa Arslan, Cüneyt Faydali, Mustafa Zengi̇n, Mustafa Küçüki̇slamoğlu, Hülya Demi̇rhan
An Efficient One Pot Synthesis Of 1,4-Dihydropyridines Using Alumina Sulfuric Acid (Asa) Catalyst, Mustafa Arslan, Cüneyt Faydali, Mustafa Zengi̇n, Mustafa Küçüki̇slamoğlu, Hülya Demi̇rhan
Turkish Journal of Chemistry
An efficient synthetic method for 1,4-dihydropyridines has been developed using 3 or 4 component condensation reactions of aldehydes, 1,3-dicarbonyl compounds, and ammonium acetate in the presence of alumina sulfuric acid catalyst in minimum methanol at reflux temperature. This procedure offers several advantages including high yields, an environmentally friendly procedure, short reaction times, and a simple work-up procedure.
Synthesis, Characterization, And Optical Properties Of Novel 2,5-Bis[4-(2-(-Arylvinyl)Phenyl]-1,3,4-Oxadiazoles, Dao-Hang He, Yong-Chuang Zhu, Zhuo-Ru Yang, Ai-Xi Hu, Gao Cao
Synthesis, Characterization, And Optical Properties Of Novel 2,5-Bis[4-(2-(-Arylvinyl)Phenyl]-1,3,4-Oxadiazoles, Dao-Hang He, Yong-Chuang Zhu, Zhuo-Ru Yang, Ai-Xi Hu, Gao Cao
Turkish Journal of Chemistry
Six novel 2,5-bis[4-(2-arylvinyl)phenyl]-1,3,4-oxadiazoles were synthesized by introducing 1,3,4-oxadiazole moiety into the stilbene skeleton. The synthesis route included the cyclization of p-toluic acid and hydrazine hydrate catalyzed by polyphosphoric acid (PPA), bromination of 1,3-dibromo-5,5-dimethylhydantoin (DBDMH), esterification, and the Wittig-Horner reaction. All the title compounds were characterized by ^1H-NMR, MS, and elemental analysis. UV-Vis absorption and fluorescence emission spectra in THF solution were investigated; the compounds may have potential for use in organic optical materials.
Synthesis And In Vitro Anti-Helicobacter Pylori Activity Of 2-(Substituted Benzylthio)-5-(5-Nitro-2- Furyl)-1, 3, 4-Thiadiazole Derivatives, Hossein Nasr Isfahani, Khalil Faghihi, Atena Izadkhah, Meisam Shabanian
Synthesis And In Vitro Anti-Helicobacter Pylori Activity Of 2-(Substituted Benzylthio)-5-(5-Nitro-2- Furyl)-1, 3, 4-Thiadiazole Derivatives, Hossein Nasr Isfahani, Khalil Faghihi, Atena Izadkhah, Meisam Shabanian
Turkish Journal of Chemistry
Starting from (5-nitrofuran-2-yl)methylene diacetate, a new series of 2-[(substituted benzyl)thio]-5-(5-nitro-2-furyl)-1,3,4-thiadiazoles (6a-n) were synthesized and the structures of the compounds were determined using spectroscopic methods including mass spectrometry, ^1H-nuclear magnetic resonance, infrared spectroscopy, and elemental analysis. The in vitro anti-Helicobacter pylori activity of the synthesized compounds was evaluated by the disk diffusion method against the clinical isolates of Helicobacter pylori. The results indicated that most of the synthesized compounds exhibited significant inhibitory activity against H. pylori with respect to standard drug metronidazole. Compound 6l, containing the 2-chloro-6-fluorobenzylthio moiety, was the most potent compound tested.
Synthesis And In Vitro Anti-Helicobacter Pylori Activity Of 2-(Substituted Benzylthio)-5-(5-Nitro-2- Furyl)-1, 3, 4-Thiadiazole Derivatives, Negar Mohammadhosseini, Ali Asadipor, Bahram Letafat, Mohsen Vosooghi, Farideh Siavoshi, Abbas Shafiee, Alireza Foroumadi
Synthesis And In Vitro Anti-Helicobacter Pylori Activity Of 2-(Substituted Benzylthio)-5-(5-Nitro-2- Furyl)-1, 3, 4-Thiadiazole Derivatives, Negar Mohammadhosseini, Ali Asadipor, Bahram Letafat, Mohsen Vosooghi, Farideh Siavoshi, Abbas Shafiee, Alireza Foroumadi
Turkish Journal of Chemistry
Starting from (5-nitrofuran-2-yl)methylene diacetate, a new series of 2-[(substituted benzyl)thio]-5-(5-nitro-2-furyl)-1,3,4-thiadiazoles (6a-n) were synthesized and the structures of the compounds were determined using spectroscopic methods including mass spectrometry, ^1H-nuclear magnetic resonance, infrared spectroscopy, and elemental analysis. The in vitro anti-Helicobacter pylori activity of the synthesized compounds was evaluated by the disk diffusion method against the clinical isolates of Helicobacter pylori. The results indicated that most of the synthesized compounds exhibited significant inhibitory activity against H. pylori with respect to standard drug metronidazole. Compound 6l, containing the 2-chloro-6-fluorobenzylthio moiety, was the most potent compound tested.