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Jean-Francois Lutz, Guillaume Fiers, Dalila Chouikhi, Laurence Oswald, Abdelaziz Al Ouahabi, Delphine Chan-Seng, Laurence Charles
Sequence-defined peptide triazole nucleic acids (PTzNA) were synthesized via a solid-phase orthogonal "AB + CD" iterative strategy. In this approach, AB and CD building blocks containing carboxylic acid (A), azide (B), alkyne (C) and primary amine (D) functions are assembled together by successive copper-catalyzed azide-alkyne cycloaddition (CuAAC) and acid-amine coupling steps. Different PTzNA genetic sequences were prepared using a library of eight building blocks (i.e. 4 AB and 4 CD building blocks).
October 18, 2016: Chemistry: a European Journal
Diego G Ghiano, Agustina de la Iglesia, Nina Liu, Peter J Tonge, Héctor R Morbidoni, Guillermo R Labadie
A collection of 1,2,3-triazoles unsaturated fatty acid mimics were efficiently synthesized by click chemistry. The 1,4-disubstituted analogs prepared covered different alkyl chain lengths and triazole positions. The compounds were subsequently tested against Mycobacterium tuberculosis, being most of them active with some of the analogs displaying activity at micromolar concentration. The most potent member of the series has the triazole moiety on the C-2 position with a carbon chain of eight or ten carbon atoms...
September 28, 2016: European Journal of Medicinal Chemistry
Camila L Madeira, Samuel A Speet, Cristina A Nieto, Leif Abrell, Jon Chorover, Reyes Sierra-Alvarez, Jim A Field
Insensitive munitions, such as 3-nitro-1,2,4-triazol-5-one (NTO), are being considered by the U.S. Army as replacements for conventional explosives. Environmental emissions of NTO are expected to increase as its use becomes widespread; but only a few studies have considered the remediation of NTO-contaminated sites. In this study, sequential anaerobic-aerobic biodegradation of NTO was investigated in bioreactors using soil as inoculum. Batch bioassays confirmed microbial reduction of NTO under anaerobic conditions to 3-amino-1,2,4-triazol-5-one (ATO) using pyruvate as electron-donating cosubstrate...
October 14, 2016: Chemosphere
Xing Wang, Zhi-Cheng Dai, Yong-Fei Chen, Ling-Ling Cao, Wei Yan, Sheng-Kun Li, Jian-Xin Wang, Zheng-Guang Zhang, Yong-Hao Ye
A series of new 1,2,3-triazole derivatives have been prepared and screened for their antifungal activity against phytopathogenic fungi using the mycelium growth inhibition method in vitro. The results indicated that the 1,2,3-triazole hydrazide scaffold displayed significant antifungal activity. Compound 6ad exhibited the most potent anti-phytopathogenic activity, with EC50 values of 0.18, 0.35, 0.37 and 2.25 μg mL(-1) against Rhizoctonia solani, Sclerotinia sclerotiorum, Fusarium graminearum, and Magnaporthe oryzae, respectively...
October 5, 2016: European Journal of Medicinal Chemistry
Petra Füredi, Zsófia Edit Pápay, Kristóf Kovács, Borbála Dalmadi Kiss, Krisztina Ludányi, István Antal, Imre Klebovich
The number of topical fungal infections is growing, mostly owing to immunosuppressive therapy. Several topical fungal infections, such as eye mycoses, can be treated by local administration of antimycotic drugs. One major group of the antifungal agents is triazole, such as voriconazole (VCZ), which is used as the first line treatment of aspergillosis. A disadvantage of VCZ is its low water solubility making the drug difficult to administer in a liquid preparation. The lipid-based nanoparticles (LNP) have attracted increasing attention due to their advantageous properties...
October 1, 2016: Journal of Pharmaceutical and Biomedical Analysis
Anupam G Banerjee, Nirupam Das, Sushant A Shengule, Piyoosh A Sharma, Radhey Shyam Srivastava, Sushant Kumar Shrivastava
A series of novel hybrids comprising of 1,3,4-oxadiazole/thiadiazole and 1,2,4-triazole tethered to 5,6-diphenyl-1,2,4-triazin-3(2H)-one were designed, synthesised and evaluated as COX-2 inhibitors for the treatment of inflammation. The synthesised hybrids were characterised using FT-IR, 1H NMR, 13C NMR, elemental (C,H,N) analyses and assessed for their anti-inflammatory potential by in vitro albumin denaturation assay. Compounds exhibiting activity comparable to indomethacin and celecoxib were further evaluated for in vivo anti-inflammatory activity...
October 11, 2016: Bioorganic Chemistry
Steven Silverman, John Moses, K Barry Sharpless
Vancomycin has long been considered a drug of last resort. Its efficiency in treating multiple drug-resistant bacterial infections, particularly methicillin resistant S. aureus (MRSA), has had a profound effect on the treatment of life-threatening infections. However, the emergence of resistance to vancomycin is a cause for significant world-wide concern, prompting the urgent development of new effective treatments for antibiotic resistant bacterial infections. Harnessing the benefits of multivalency and cooperativity against vancomycin-resistant strains, we report a Click Chemistry approach towards reengineered vancomycin derivatives and the synthesis of a number of dimers with increased potency against MRSA and vancomycin resistant Enterococci (VRE)...
October 16, 2016: Chemistry: a European Journal
James R Wright, James D Crowley, Nigel T Lucas
Hexaphenylbenzene (HPB) and hexa-peri-hexabenzocoronene-(HBC) functionalised 1,2,3-triazoles have been synthesised using an optimised copper(i)-catalysed azide-alkyne cycloaddition (CuAAC) reaction. The coordination chemistry of these ligands was explored through the synthesis of the respective palladium(ii) complexes and their activity as catalysts in the Suzuki-Miyaura reaction assessed.
October 17, 2016: Chemical Communications: Chem Comm
Siddiq Pasha Shaik, V Lakshma Nayak, Faria Sultana, A V Subba Rao, Anver Basha Shaik, Korrapati Suresh Babu, Ahmed Kamal
A series of imidazo[2,1-b]thiazole linked triazole conjugates were synthesized by using Huisgen 1,3-dipolar cyclo-addition reaction (click chemistry approach) and evaluated for their antiproliferative activity against some human cancer cell lines like, HeLa (cervical), DU-145 (prostate), A549 (lung), MCF-7 (breast) and HepG2 (liver). Among them, Conjugates 4g and 4h demonstrated a significant antiproliferative effect against human lung cancer cells (A549) with IC50 values of 0.92 and 0.78 μM respectively...
September 20, 2016: European Journal of Medicinal Chemistry
Julie M Muller, Shane S Galley, Thomas E Albrecht-Schmitt, Kenneth L Nash
The complexation of selected trivalent lanthanide ions with derivatives of the tetranitrogen donor ligands 6,6'-bis-1R,1H-1,2,3-triazol-4-yl-2,2'-bipyridines (BTzBPs, R = alkyl or aryl) was investigated in solid state and in solution. An anhydrous solid [Ce(Bn-BTzBP)(NO3)3] (Bn = benzene) complex was synthesized and characterized by single-crystal X-ray diffraction. Eu(III) complexes with the 2-ethyl(hexyl) derivative EH-BTzBP in methanol were studied by time-resolved fluorescence spectroscopy. Earlier studies have identified the EH-BTzBP as a potentially useful solvent extraction reagent for the separation of americium from lanthanide metal ions, a challenging component of advanced nuclear fuel cycles for actinide transmutation...
October 14, 2016: Inorganic Chemistry
D Madea, T Slanina, P Klán
A bioorthogonal 'catch and photorelease' strategy, which combines alkyne-azide cycloaddition between p-hydroxyphenacyl azide and alkyne derivatives to form a 1,2,3-triazole adduct and subsequent photochemical release of the triazole moiety via a photo-Favorskii rearrangement, is introduced. The first step can also involve photorelease of a strained alkyne and its Cu-free click reaction with azide.
October 14, 2016: Chemical Communications: Chem Comm
M Chaâbane, I Ghorbel, A Elwej, H Mnif, T Boudawara, S Ellouze Chaâbouni, N Zeghal, N Soudani
Pesticides exposure causes usually harmful effects to the environment and human health. The present study aimed to investigate the potential toxic effects of penconazole, a triazole fungicide, on the cerebrum and cerebellum of adult rats. Penconazole was administered intraperitoneally to male Wistar rats at a dose of 67 mg kg(-1) body weight every 2 days during 9 days. Results showed that penconazole induced oxidative stress in rat cerebrum and cerebellum tissues. In fact, we have found a significant increase in malondialdehyde, hydrogen peroxide, and advanced oxidation protein product levels, as well as an alteration of the antioxidant status, enzymatic (superoxide dismutase and catalase) and nonenzymatic (glutathione), the cholinergic function, and membrane-bound ATPases (Na(+)/K(+)-ATPase and Mg(2+)-ATPase)...
October 12, 2016: Human & Experimental Toxicology
Christopher J Brassard, Xiaoguang Zhang, Christopher R Brewer, Peiye Liu, Ronald J Clark, Lei Zhu
Copper(II) acetate under aerobic conditions catalyzes the formation of 5,5'-bis(1,2,3-triazole)s (5,5'-bistriazoles) from organic azides and terminal alkynes. This reaction is an oxidative extension of the widely used copper-catalyzed azide-alkyne 'click' cycloaddition. The inclusions of potassium carbonate as an additive and methanol or ethanol as the solvent, and in most instances an atmosphere of dioxygen, promote the oxidative reaction to afford 5,5'-bistriazole at the expanse of 5-protio-1,2,3-triazole (5-protiotriazole)...
October 14, 2016: Journal of Organic Chemistry
Babita Aneja, Mohammad Irfan, Charu Kapil, Mohamad Aman Jairajpuri, Ronan Maguire, Kevin Kavanagh, M Moshahid A Rizvi, Nikhat Manzoor, Amir Azam, Mohammad Abid
The increasing incidence of human candidiasis and the tendency of Candida species to become resistant to existing chemotherapies are well-recognized health problems. The present study demonstrates the successful synthesis of novel triazole-amino acid hybrids with potent in vitro and in vivo inhibitory activity against Candida species. Particularly, compounds 68 and 70 showed potent in vitro activity against fluconazole (FLC) resistant as well as sensitive clinical isolates of Candida albicans. Time kill curve analysis of lead inhibitors 68 and 70 showed their fungistatic nature...
October 13, 2016: Organic & Biomolecular Chemistry
Paula Regina Elias, Gleicekelly Silva Coelho, Viviane Flores Xavier, Policarpo Ademar Sales Junior, Alvaro José Romanha, Silvane Maria Fonseca Murta, Claudia Martins Carneiro, Nilton Soares Camilo, Flaviane Francisco Hilário, Jason Guy Taylor
A series of novel xylitan derivatives derived from xylitol were synthesized using operationally simple procedures. A xylitan acetonide was the key intermediate used to prepare benzoate, arylsulfonate esters and 1,2,3-triazole derivatives of xylitan. These compounds were evaluated for their in vitro anti-Trypanosoma cruzi activity against trypomastigote and amastigote forms of the parasite in T. cruzi-infected cell lineages. Benznidazole was used as positive control against T. cruzi and cytotoxicity was determined in mammalian L929 cells...
October 10, 2016: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
Qizhen Wei, Zhiyu Song, Jing Nie, Hailun Xia, Fujiang Chen, Zuguang Li, Mawrong Lee
A pretreatment method named tablet-effervescence-assisted dissolved carbon flotation was introduced for the determination of four triazole fungicides in environmental water. In this method, the use of effervescent tablet composed of nontoxic sodium carbonate and sodium dihydrogen phosphate could generate CO2 in situ to assist the dispersion of extraction solvent and to accelerate mass transfer of target analytes. In addition, the simple phase separation simply based on the rising of low-density organic solvent from the aqueous phase was applied rather than the application of apparatus, which demonstrated the potential for on-site extraction in the field...
October 13, 2016: Journal of Separation Science
Santiago Rodríguez-Jiménez, Humphrey L C Feltham, Sally Brooker
Materials capable of sensing volatile guests at room temperature by an easily monitored set of outputs are of great appeal for development as chemical sensors of small volatile organics and toxic gases. Herein the dinuclear iron(II) complex, [Fe(II)2 (L)2 (CH3 CN)4 ](BF4 )4 ⋅2 CH3 CN (1) [L=4-(4-methylphenyl)-3-(3-pyridazinyl)-5-pyridyl-4H-1,2,4-triazole], is shown to undergo reversible single-crystal-to-single-crystal (SCSC) transformations upon exposure to vapors of different guests: 1 (MeCN)⇌2 (EtOH)→3 (H2 O)⇌1 (MeCN)...
October 12, 2016: Angewandte Chemie
Papigani Neeraja, Suryapeta Srinivas, Khagga Mukkanti, Pramod Kumar Dubey, Sarbani Pal
1H-1,2,3-Triazolyl-substituted 1,3,4-oxadiazole derivatives containing structural features of ibuprofen/naproxen were synthesized for the first time using a Cu catalyzed azide-alkyne cycloaddition (CuAAC) strategy. An optimized reaction condition was established for this purpose and twenty new compounds were synthesized using this methodology. Several of these compounds showed good to reasonable antibacterial activities when tested against three gram-positive and three gram-negative species. The compound 4m i...
September 25, 2016: Bioorganic & Medicinal Chemistry Letters
Liya D Funt, Olesya A Tomashenko, Alexander F Khlebnikov, Mikhail Sergeevich Novikov, Alexander Yu Ivanov
Unprecedented pyrrole- and 1,2,4-triazole-containing ensembles, substituted 1-(1H-pyrrol-3-yl)-4H-1,2,4-triazol-1-ium bromides and 4-(1H-pyrrol-3-yl)-1H-1,2,4-triazol-4-ium bromides, were prepared from 2H-azirines and triazolium phenacyl bromides using a simple procedure. N-(1H-Pyrrol-3-yl)-N'-benzyltriazolium bromides undergo reductive debenzylation on Pd/C to give substituted 1-(1H-pyrrol-3-yl)-4H-1,2,4-triazoles and 4-(1H-pyrrol-3-yl)-1H-1,2,4-triazoles in high yields. Betaines (triazoliumylpyrrolides) and pyrrolyltriazole NHCs, which are possible products of dehydrobromination of pyrrolyltriazolium salts, have comparable thermodynamic stabilities in nonpolar solvents according to the calculations at the DFT B3LYP/6-31G(d) level...
October 11, 2016: Journal of Organic Chemistry
Fang Yao, Zhi-Yu Song, Jing Nie, Zu-Guang Li, Guo-Hua Zhu, Maw-Rong Lee
A novel dissolved carbon dioxide flotation after emulsification microextraction (DCF-EME) method was proposed for the determination of four triazole pesticides in water samples coupled with gas chromatography-mass spectrometry (GC-MS) in a home-made glass round flask. The DCF-EME method is based on a rapid and simple phase separation of low-density organic solvent (toluene) from the aqueous phase via introducing a saturated NaHCO3 solution into the acidified sample (0.1 mol L(-1) HCl); then analytes were extracted in toluene...
2016: Analytical Sciences: the International Journal of the Japan Society for Analytical Chemistry
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