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Alessandro Sinopoli, Fiona A Black, Christopher J Wood, Elizabeth A Gibson, Paul I P Elliott
A novel anchoring ligand for dye-sensitised solar cell chromophoric complexes, 1-(2,2'-bipyrid-4-yl)-1,2,3-triazole-4,5-dicarboxylic acid (dctzbpy), is described. The new dye complexes [Ru(bpy)2(dctzbpy)][PF6]2 (AS16), [Ir(ppy)2(dctzbpy)][PF6] (AS17) and [Re(dctzbpy)(CO)3Cl] (AS18) were prepared in a two stage procedure with intermediate isolation of their diester analogues, AS16-Et2, AS17-Et2 and AS18-Et2 respectively. Electrochemical analysis of AS16-Et2, AS17-Et2 and AS18-Et2 reveal reduction potentials in the range -1...
January 16, 2017: Dalton Transactions: An International Journal of Inorganic Chemistry
Jacques F Meis, Anuradha Chowdhary, Johanna L Rhodes, Matthew C Fisher, Paul E Verweij
Aspergillus fungi are the cause of an array of diseases affecting humans, animals and plants. The triazole antifungal agents itraconazole, voriconazole, isavuconazole and posaconazole are treatment options against diseases caused by Aspergillus However, resistance to azoles has recently emerged as a new therapeutic challenge in six continents. Although de novo azole resistance occurs occasionally in patients during azole therapy, the main burden is the aquisition of resistance through the environment. In this setting, the evolution of resistance is attributed to the widespread use of azole-based fungicides...
December 5, 2016: Philosophical Transactions of the Royal Society of London. Series B, Biological Sciences
Shui-Xiu Li, Yan-Jun Song, Ling Jiang, Ya-Jing Zhao, Hui Guo, Dong-Mei Li, Kun-Ju Zhu, Hong Zhang
In our earlier in vitro and in vivo studies, synergistic effects were observed when itraconazole or voriconazole were combined with tetrandrine (TET) against Aspergillus fumigatus, and the synergistic mechanism was related to inhibition of the drug efflux pump. Posaconazole (PCZ) is a broad-spectrum triazole antifungal agent used for the treatment of diverse fungal infections, including aspergillosis and candidiasis. Herein, the antifungal effects of TET are further investigated in vitro and in vivo alone or combined with PCZ against 20 clinical isolates of A...
January 12, 2017: Microbial Drug Resistance: MDR: Mechanisms, Epidemiology, and Disease
Dengke Li, Tingting Mao, Jinbo Huang, Qiang Zhu
An efficient approach to prepare 1,2,3-triazolo[1,5-a]quinoxaline scaffolds, starting from 1-azido-2-isocyanoarenes and terminal acetylenes or substituted acetaldehydes, has been developed. In the case of trifluoromethylation triggered cyclization, four chemical bonds, including two C-C and two C-N bonds, were formed consecutively without isolating the triazole intermediate. In addition, these triazo-fused products were readily transformed into diversified quinoxaline derivatives via rhodium-catalyzed carbenoid insertion reactions...
January 10, 2017: Chemical Communications: Chem Comm
Da-Wei Zhang, Yu-Min Zhang, Jing Li, Tian-Qi Zhao, Qiang Gu, Feng Lin
An efficient synthesis of 1,4-disubstituted 1,2,3-triazole derivatives was studied. 1,4-Disubstituted 1,2,3-triazoles containing isoxazole and thymidine structures were synthesized in 84-96% yields starting from various terminal isoxazole ether alkynes and β-thymidine azide derivatives via a 1,3-dispolar cycloaddition using copper acetate, sodium ascorbate as the catalyst under ultrasonic assisted condition. All the target compounds were characterized by HRMS, FT-IR, (1)H NMR and (13)C NMR spectroscopy. Furthermore, the quorum sensing inhibitory activities of synthesized compounds were evaluated with Chromobacterium violaceum (C...
May 2017: Ultrasonics Sonochemistry
Baiju P Krishnan, Kana M Sureshan
Though topochemical reactions are attractive, the difficulty associated with crystallization such as low yield, unsuitability for large scale synthesis etc warranted the exploitation of other self-assembled media for topochemical reactions. We synthesized a dipeptide gelator decorated with azide and alkyne at its termini, N3-Ala-Val-NHCH2-C≡CH, which is designed to self-assemble through intermolecular hydrogen bonds to β-sheets thereby placing the azide and alkyne motifs at proximity. As anticipated, this peptide forms gels in organic solvents and water via hydrogen-bonded β-sheet assembly as evidenced from IR spectroscopy and PXRD profiling...
January 10, 2017: Journal of the American Chemical Society
Elaine Armelin, Rory Whelan, Yeimy Mabel Martínez-Triana, Carlos Aleman, M G Finn, David Diaz Diaz
Organic polymers are widely used as coatings and adhesives to metal surfaces, but aluminum is among the most difficult substrates because of rapid oxidative passivation of its surface. Poly(1,4-disubstituted 1,2,3-triazoles) made by copper-catalyzed azide-alkyne cycloaddition form strongly bonded interfaces with several metal substrates. In this work, a variety of alkyne and azide monomers were explored as precursors to anticorrosion coatings for a standard high-strength aluminum-copper alloy. Monomers of comparatively low valency (diazide and trialkyne) were found to act as superior barriers for electrolyte transfer to the aluminum surface...
January 9, 2017: ACS Applied Materials & Interfaces
Amol M Vibhute, Poornenth Pushpanandan, Maria Varghese, Vera Koniecnzy, Colin W Taylor, Kana M Sureshan
Inositol 1,4,5-trisphosphate receptors (IP3Rs) are tetrameric intracellular channels through which many extracellular stimuli initiate the Ca(2+) signals that regulate diverse cellular responses. There is considerable interest in developing novel ligands of IP3R. Adenophostin A (AdA) is a potent agonist of IP3R and since some dimeric analogs of IP3R ligands are more potent than the corresponding monomer; we considered whether dimeric AdA analogs might provide agonists with increased potency. We previously synthesized traizolophostin, in which a simple triazole replaced the adenine of AdA, and showed it to be equipotent to AdA...
November 3, 2016: RSC Advances
Cuimei Liu, Wei Jia, Zhendong Hua, Zhenhua Qian
Clinical and forensic toxicology laboratories are continuously confronted by analytical challenges when dealing with the new psychoactive substances phenomenon. The number of synthetic cannabinoids, the chemical diversity, and the speed of emergence make this group of compounds particularly challenging in terms of detection, monitoring, and responding. Three indazole 7 N positional isomer synthetic cannabinoids, two ethyl 2-amino-3-methylbutanoate-type synthetic cannabinoids, and one 9H-carbazole substituted synthetic cannabinoid were identified in seized materials...
January 7, 2017: Drug Testing and Analysis
T V Soumya, C Muhammed Ajmal, D Bahulayan
An easy synthetic protocol for the peptide randomization of 3,5-dicyano pyridine derivatives by linking the pyridine core with a coumarin chromophore spaced by a linker triazole via copper (I) catalyzed [3+2] azide-alkyne cycloaddition (CuAAC) is described. The new peptidomimetics thus obtained are extended rule of 5 (eRo5) molecules suitable for the development of therapeutic agents for undruggable targets. The structural and photophysical properties of the molecules are also promising for the development of potential bio imaging agents based on these molecules...
December 18, 2016: Bioorganic & Medicinal Chemistry Letters
Alan J Kennedy, Aimee R Poda, Nicolas L Melby, Lee C Moores, Shinita M Jordan, Kurt A Gust, Anthony J Bednar
Insensitive munitions (IMs) are desirable alternatives to historically used formulations, such as 2,4,6-trinitrotoluene (TNT), due to their "insensitivity" to unintended detonation. The insensitive munition IMX-101 is a mixture of 2,4-dinitroanisole (DNAN), 3-nitro-1,2,4-triazol-5-one (NTO), and nitroguanidine (NQ). Environmental releases of munitions may be from production wastewaters or training; these munitions may be exposed to Ultraviolet light. Therefore, it is useful to understand the relative toxicity of IMX-101 and its constituents both before and after photo-degradation...
January 6, 2017: Environmental Toxicology and Chemistry
Cheryl Allen, Sandhya Kortagere, Huaxiang Tong, Robert A Matthiesen, Joseph I Metzger, David F Wiemer, Sarah A Holstein
The isoprenoid donor for protein geranylgeranylation reactions, geranylgeranyl diphosphate (GGDP), is the product of the enzyme GGDP synthase (GGDPS) which condenses farnesyl diphosphate (FDP) and isopentenyl pyrophosphate. GGDPS inhibition is of interest from a therapeutic perspective for multiple myeloma as we have shown that targeting Rab GTPase geranylgeranylation impairs monoclonal protein trafficking, leading to endoplasmic reticulum stress and apoptosis. We have reported a series of triazole bisphosphonate GGDPS inhibitors of which the most potent was a 3:1 mixture of homogeranyl (HG) and homoneryl (HN) isomers...
January 5, 2017: Molecular Pharmacology
Kriti Acharya, Adel A Rashad, Francesca Moraca, Per Johan Klasse, John P Moore, Cameron Abrams, Irwin Chaiken
Peptide triazole (PT) antagonists interact with gp120 subunits of HIV-1 Env trimers to block host cell receptor interactions, trigger gp120 shedding, irreversibly inactivate virus and inhibit infection. Despite these enticing functions, understanding the structural mechanism of PT-Env trimer encounter has been limited. In this work, we combined competition interaction analysis and computational simulation to demonstrate PT binding to the recombinant soluble trimer, BG505 SOSIP.664, a stable variant that resembles native virus spikes in binding to CD4 receptor as well as known conformationally-dependent Env antibodies...
January 5, 2017: Proteins
Mohammed A E Sallam
Dehydrative cyclization of 4-(D-altro-pentitol-1-yl)2-phenyl-2H-1,2,3-triazole in basic medium with one moler equivalent of p-toluene sulfonyl chloride in pyridine solution gave the homo-C-nucleoside 4-(2,5-anhydro-D-altro-1-yl)-2-phenyl-2H-1,2,3-triazole. The structure and anomeric configuration was determined by acylation, nuclear magnetic resonance (NMR), and mass spectroscopy. The stereochemistry at the carbon bridge of homo-C-nucleoside 2-phenyl-2H-1,2,3-triazoles was determined by circular dichroism (CD) spectroscopy...
January 2017: Chirality
Shashir Wanjare, Rajarshi Gupta, Preeti Mehta
INTRODUCTION: Emergence of Candida species resistant to Amphotericin B and triazole has led to use of echinocandins, mostly caspofungin in the management of invasive candidiasis. There are some published reports of caspofungin resistance in Candida species yet no studies on caspofungin susceptibility pattern of Candida species exist in Indian setup. AIM: To carry out the antifungal susceptibility of Candida isolates against caspofungin. MATERIALS AND METHODS: In a retrospective study at a tertiary care teaching hospital, 60 preserved Candida isolates from inpatients of invasive candidiasis obtained over a period of 6 months from January 2015 to June 2015 were subjected to antifungal susceptibility to caspofungin and the Minimum Inhibitory Concentrations (MICs) of Candida species to caspofungin were determined by Epsilometer test (E-test)...
November 2016: Journal of Clinical and Diagnostic Research: JCDR
Guoqing Sui, Wen Zhang, Kun Zhou, Yulin Li, Bingyu Zhang, Dan Xu, Yong Zou, Wenming Zhou
As a part of our continuing research on amine derivative antifungal agents, 19 novel target compounds containing 1,2,4-triazole and tertiary amine moieties were designed and synthesized, and their in vitro antifungal activities against six phytopathogenic fungi (Magnaporthe grisea, Alternaria solani, Fusarium solani, Curvularia lunata, A. alternata, F. graminearum) were assayed. All target compounds were elucidated by means of (1)H-NMR, (13)C-NMR, high resolution (HR)-MS, and IR analysis. The results showed that most of the derivatives exhibited obvious activity against each of the fungi at 50 µg/mL...
2017: Chemical & Pharmaceutical Bulletin
Zaineb A F Albayati, Venumadhav Janganati, Zheng Chen, Jessica Ponder, Philip J Breen, Craig T Jordan, Peter A Crooks
A series of carbamate derivatives of the antileukemic sesquiterpene melampomagnolide B (MMB) has been synthesized utilizing a 1,2,4-triazole carbamate conjugate of MMB as an intermediate synthon. Five imidazole- and benzimidazole-carbamate analogs of MMB (8a-8e) were prepared and evaluated for anti-leukemic activity against cultured M9 ENL1 AML cells. All the analogs exhibited improved anti-leukemic activity (EC50=0.90-3.93μM) when compared to parthenolide and the parent sesquiterpene, MMB (EC50=7.0μM and 15...
December 26, 2016: Bioorganic & Medicinal Chemistry
Wei Chen, Ya-Li Bai, Yong-Chun Luo, Peng-Fei Xu
A novel strategy was developed for the application of Rh carbenes generated from readily accessible N-sulfonyl 1,2,3,-triazoles or diazocompouds in the high order cycloadditions, which offered an efficient route to a variety of N-containing medium-sized rings. The process provided a wide range of cyclohepta[b]pyrazine and cyclohepta[b]pyrrolone derivatives with high yields.
January 3, 2017: Organic Letters
Moondra Zubir, Atom Hamasaki, Taku Iiyama, Akira Ohta, Hiroshi Ohki, Sumio Ozeki
As-synthesized [Zn2(Oxac)(Taz)2]•(H2O)2.5, referred to ZOTW2.5, was prepared from aqueous methanol solutions of Zn5(CO3)2(OH)6 and two kinds of ligands of 1,2,4-triazole (Taz) and oxalic acid (Oxac) at 453 K for 12 hours. The crystal structure was determined by the Rietveld method. The as-synthesized ZOTW2.5 was pretreated at 383 K and 1 mPa for tpt h, ZOTWx(tpth). ZOTWx(≥3h) showed Type I adsorption isotherm for N2 at 77 K having the saturation amount (Vs) of 180 mg/g, but that pretreated shortly showed only 1/10 in Vs...
January 3, 2017: Langmuir: the ACS Journal of Surfaces and Colloids
Michael J Murphy, Katrina A Zenere, Florence Ragon, Peter David Southon, Cameron John Kepert, Suzanne M Neville
The spin crossover (SCO) phenomenon defines an elegant class of switchable materials that can show cooperative transitions when long-range elastic interactions are present. Such materials can show multi-stepped transitions, targeted both fundamentally and for expanded data storage applications, when antagonistic interactions (i.e., competing ferro- and antiferro-elastic interactions) drive concerted lattice distortions. To this end, a new SCO framework scaffold, [FeII(bztrz)2(PdII(CN)4)]·n(guest) (bztrz = (E)-1-phenyl-N-(1,2,4-triazol-4-yl)methanimine, 1·n(guest)), has been prepared that supports a variety of antagonistic solid state interactions alongside a distinct dual guest pore system...
January 3, 2017: Journal of the American Chemical Society
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