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Beena Negi, Prija Poonan, Mohammad Fawad Ansari, Deepak Kumar, Sakshi Aggarwal, Ramandeep Singh, Amir Azam, Diwan S Rawat
A series of 22 novel metronidazole-triazole-styryl hybrids were synthesized and evaluated for their in vitro antiamoebic activity against HM1: IMSS strain of Entamoeba histolytica. Some of the hybrids were found to be more active (IC50  = 0.12-0.35 μM) than the reference drug metronidazole (IC50  = 1.79 μM). The most active compounds were found to be non-toxic (up to 50 μM) against the Vero cells showing a good safety profile of these hybrids. The docking and ADMET studies were also conducted to investigate the probable mode of action...
March 13, 2018: European Journal of Medicinal Chemistry
Çinel Köksal Karayildirim, Mustafa Kotmakçi, Erkan Halay, Kadir Ay, Yücel Başpinar
5-Fluorouracil is one of the first line drugs for the systemic therapy of solid tumors like breast, colorectal, oesophageal, stomach, pancreatic, head and neck. It could be shown that sugars can improve the absorption across cell membranes and can help to bypass some pharmacokinetic problems. Carbohydrates as most common organic molecules are an important issue of plant and animal metabolisms. They are non toxic and have important duties in the body like participating in DNA and RNA synthesis and being responsible for energy production...
March 2018: Saudi Pharmaceutical Journal: SPJ: the Official Publication of the Saudi Pharmaceutical Society
Scott R Gilbertson, Ying-Chu Chen, Claudia A Soto, Yaxing Yang, Kenner C Rice, Kathryn A Cunningham, Noelle C Anastasio
The approach of tethering together two known receptor ligands, to be used as molecular probes for the study of G protein-coupled receptor (GPCR) systems, has proven to be a valuable approach. Selective ligands that possess functionality that can be used to link to other ligands, are useful in the development of novel antagonists and agonists. Such molecules can also be attached to reporter molecules, such as fluorophores, for the study of GPCR dimerization and its role in signaling. The highly selective serotonin (5-HT) 5-HT2A receptor (5-HT2A R) antagonist M100907 (volinanserin) is of clinical interest in the treatment of neurological and mental health disorders...
March 16, 2018: Bioorganic & Medicinal Chemistry Letters
Caitlin R Rausch, Dimitrios P Kontoyiannis
Voriconazole is a triazole antifungal with activity against a number of yeast and mold species including Candida, Aspergillosis, Fusarium, and Coccidioides. Invasive fungal infections are associated with high morbidity and mortality, prolonged treatment courses, and occasionally lifelong suppressive therapy. Voriconazole therapy can result in a number of acute toxicities that clinicians are frequently aware of including hepatotoxicity, visual disturbances, and hallucinations; however, there is limited experience with extended durations of voriconazole therapy...
January 1, 2018: Journal of Oncology Pharmacy Practice
Yanshuai Xing, Xiaoshuang Meng, Lei Wang, Junjie Zhang, Zijing Wu, Xinying Gong, Chenye Wang, Hongwen Sun
Triazole contaminants in water and soil environments can form complexes with metal ions, and therefore affect the bioavailability and toxicity of some heavy metals. In present study, significant increase of copper (Cu) uptake by earthworm (Eisenia fetida) was observed when combined pollution of benzotriazole (BTR) presented in soil. For instance, Cu accumulation in earthworms increased 55% approximately when BTR presented at the BTR/Cu molar ratio of 1:2.5. While the single Cu exposure (at 32 mg kg-1 in soil) resulted in increased malondialdehyde (MDA) content in earthworms from 0...
March 12, 2018: Journal of Hazardous Materials
Meng-Ting Li, Xi-Ya Yang, Ji-Sen Li, Ning Sheng, Guo-Dong Liu, Jing-Quan Sha, Ya-Qian Lan
For exploring the multifold helical fabrication of polyoxometalate (POM)-based hybrid compounds, four POM-based crystalline compounds with different meso-helices, H3 [Ag27 (trz)16 (H2 O)6 ][SiW12 O40 ]2 ·5H2 O (1), H[Ag27 (trz)16 (H2 O)4 ][PW12 O40 ]2 ·2H2 O (2), [Ag23 (trz)14 (H2 O)2 ][HSiW12 O40 ] (3), and [Ag23 (trz)14 (H2 O)2 ][PW12 O40 ] (4), were successfully isolated by using the delicate 1,2,3-triazole ligand and silver ions in this work. Crystal analysis reveals that compounds 1 and 2 and compounds 3 and 4 are isomorphous and display 2-/4-fold mixed meso-helices and simple 2-fold meso-helices, respectively...
March 19, 2018: Inorganic Chemistry
Sreejesh Sreedharan, Alessandro Sinopoli, Paul J Jarman, Darren Robinson, Christopher Clemmet, Paul A Scattergood, Craig R Rice, Carl G W Smythe, James A Thomas, Paul I P Elliott
Two new biscyclometalated complexes [Ir(ptzR)2(dppz)]+ (dppz = dipyridophenazene; ptzRH = 4-phenyl-1-benzyl-1,2,3-triazole (1+) and 4-phenyl-1-propyl-1,2,3-triazole (2+)) have been prepared. The hexafluorophosphate salts of these complexes have been fully characterized and, in one case, the X-ray structure of a nitrate salt was obtained. The DNA binding properties of the chloride salts of the complexes were investigated, as well as their cellular uptake by A2780 and MCF7 cell lines. Both complexes display an increase in the intensity of phosphorescence upon titration with duplex DNA, indicating the intercalation of the dppz ligand and, given that they are monocations, the complexes exhibit appreciable DNA binding affinity...
March 19, 2018: Dalton Transactions: An International Journal of Inorganic Chemistry
M-P Ledoux, J Denis, Y Nivoix, R Herbrecht
Isavuconazole, the active moiety of its prodrug isavuconazonium, is a new extended-spectrum triazole whose activity against yeasts, molds, including Aspergillus and mucorales, and dimorphic fungi has been shown in vitro and in preclinical models. The most relevant pharmacokinetics features are water-solubility of the prodrug, rapid cleavage of the prodrug into active moiety and cleavage product by plasmatic esterases, high oral bioavailability of isavuconazole with an extensive penetration into most tissues and a good safety profile even in case of renal impairment...
March 15, 2018: Journal de Mycologie Médicale
Boddu Rama Krishna, Dinesh Thummuri, V G M Naidu, Sistla Ramakrishna, Uppuluri Venkata Mallavadhani
A total of twenty-two novel coumarin triazole hybrids (4a-4k and 6a-6k) were synthesized from orcinol in good to excellent yields of 70-94%. The structures of all the synthesized compounds were elucidated by spectroscopic techniques such as1 H NMR,13 C NMR, and HRMS. The anti-inflammatory potential of synthesized compounds was investigated against the proinflammatory cytokine, TNF-α on U937 cell line and compounds 4d, 4j, and 6j were found to exhibit promising anti-inflammatory activity. These three compounds were further screened against TNF-α on LPS-stimulated RAW 264...
March 7, 2018: Bioorganic Chemistry
Leila Dehestani, Nematollah Ahangar, Seyedeh Mahdieh Hashemi, Hamid Irannejad, Patrick Honarchian Masihi, Aidin Shakiba, Saeed Emami
A series of phenacyl triazole hydrazones 3 have been designed based on the hybridization of (arylalkly)triazole and aroyl hydrazone scaffolds as new anticonvulsant agents. The target compounds 3 were easily synthesized from appropriate phenacyl triazoles and aryl acid hydrazides and characterized by IR, NMR and Mass spectroscopy. The in vivo anticonvulsant evaluation of synthesized compounds by using MES and PTZ tests revealed that they are more effective in MES model respect to PTZ test. All compounds showed 33-100% protection against MES-induced seizures at the dose of 100 mg/kg...
March 7, 2018: Bioorganic Chemistry
Sándor Kun, Éva Bokor, Ádám Sipos, Tibor Docsa, László Somsák
The aim of the present study was to broaden the structure-activity relationships of C - and N -β-d-glucopyranosyl azole type inhibitors of glycogen phosphorylase. 1-Aryl-4-β-d-gluco-pyranosyl-1,2,3-triazoles were prepared by copper catalyzed azide-alkyne cycloadditions between O -perbenzylated or O -peracetylated β-d-glucopyranosyl ethynes and aryl azides. 1-β-d-Gluco-pyranosyl-4-phenyl imidazole was obtained in a glycosylation of 4(5)-phenylimidazole with O -peracetylated α-d-glucopyranosyl bromide. C -β-d-Glucopyranosyl- N -substituted-tetrazoles were synthesized by alkylation/arylation of O -perbenzoylated 5-β-d-glucopyranosyl-tetrazole or from a 2,6-anhydroheptose tosylhydrazone and arenediazonium salts...
March 15, 2018: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
Geraldine Dowling, Pierce V Kavanagh, Hans-Georg Eckhardt, Brendan Twamley, Gary Hessman, Gavin McLaughlin, John O' Brien, Simon D Brandt
Nitrazolam and clonazolam are two designer benzodiazepines that are available from internet retailers and there is growing evidence suggesting that such compounds have the potential to cause severe adverse events. Information about tolerability in humans is scarce but typically, low doses can be difficult to administer for users when handling bulk material and variability of the active ingredient in tablet formulations can also be of a concern. Customs, toxicology and forensic laboratories are increasingly encountering designer benzodiazepines, both in tablet and powdered forms, and the unavailability of reference standards can impact on the ability to identify these compounds...
March 15, 2018: Drug Testing and Analysis
Yuan Zhang, Vijai Kumar Reddy Tangadanchu, Yu Cheng, Ren-Guo Yang, Jian-Mei Lin, Cheng-He Zhou
A series of isopropanol-bridged carbazole azoles as potential antimicrobial agents were designed and synthesized from commercial carbazoles. Bioassay revealed that 3,6-dichlorocarbazolyl triazole 3f could effectively inhibit the growth of E. faecalis with minimal inhibitory concentration of 2 μg/mL. The active molecule 3f showed lower propensity to trigger the development of resistance in bacteria than norfloxacin and exerted rapidly bactericidal ability. Compound 3f also exhibited low cytotoxicity to normal mammalian RAW264...
March 8, 2018: ACS Medicinal Chemistry Letters
Jacek Mularski, Barbara Czaplińska, Wioleta Cieślik, Jakub Bebłot, Piotr Bartczak, Rafał Sitko, Jarosław Polański, Robert Musiol
Electrolytic copper is a well-known form of pure, oxygen free copper that is used for industrial applications. In this work, the catalytic potential of this relatively cheap material was studied. The addition of less than 0.015 mol equivalent of copper powder effectively catalysed the one-pot synthesis of triazoles from a diverse range of organic halides and alkynes. Quantitative conversions in aqueous solvents can be achieved within minutes. The heterogenous nature of the catalyst afforded a low level of copper contamination in the products, thus meeting the rigorous criteria of the pharmaceutical industry...
March 14, 2018: Scientific Reports
Agustin Resendiz Sharpe, Katrien Lagrou, Jacques F Meis, Anuradha Chowdhary, Shawn R Lockhart, Paul E Verweij
Triazole resistance is an increasing concern in the opportunistic mold Aspergillus fumigatus. Resistance can develop through exposure to azole compounds during azole therapy or in the environment. Resistance mutations are commonly found in the Cyp51A-gene, although other known and unknown resistance mechanisms may be present. Surveillance studies show triazole resistance in six continents, although the presence of resistance remains unknown in many countries. In most countries, resistance mutations associated with the environment dominate, but it remains unclear if these resistance traits predominately migrate or arise locally...
April 1, 2018: Medical Mycology: Official Publication of the International Society for Human and Animal Mycology
Vladimir Motornov, Athanasios Markos, Petr Beier
A rhodium-catalyzed transannulation via ring-opening of N-(per)fluoroalkyl-substituted 1,2,3-triazoles followed by cycloaddition with different nitriles, enol ethers, isocyanates and silyl ketene acetals under microwave heating provided a highly efficient route to previously unreported N-(per)fluoroalkyl-substituted imidazoles, pyrroles, imidazolones and pyrrolones, respectively. These reactions were found to be applicable to the synthesis of a variety of 5-membered heterocycles bearing different (per)fluoroalkyl substituents as well as both electron-donating and electron-withdrawing groups attached to the heterocyclic core...
March 14, 2018: Chemical Communications: Chem Comm
Sylwia Bloch, Bożena Nejman-Faleńczyk, Karolina Pierzynowska, Ewa Piotrowska, Alicja Węgrzyn, Christelle Marminon, Zouhair Bouaziz, Pascal Nebois, Joachim Jose, Marc Le Borgne, Luciano Saso, Grzegorz Węgrzyn
Oxidative stress may be the major cause of induction of Shiga toxin-converting (Stx) prophages from chromosomes of Shiga toxin-producing Escherichia coli (STEC) in human intestine. Thus, we aimed to test a series of novel antioxidant compounds for their activities against prophage induction, thus, preventing pathogenicity of STEC. Forty-six compounds (derivatives of carbazole, indazole, triazole, quinolone, ninhydrine, and indenoindole) were tested. Fifteen of them gave promising results and were further characterized...
December 2018: Journal of Enzyme Inhibition and Medicinal Chemistry
Francesco Manzoni, Ulf Ryde
We have calculated relative binding affinities for eight tetrafluorophenyl-triazole-thiogalactoside inhibitors of galectin-3 with the alchemical free-energy perturbation approach. We obtain a mean absolute deviation from experimental estimates of only 2-3 kJ/mol and a correlation coefficient (R2 ) of 0.5-0.8 for seven relative affinities spanning a range of up to 11 kJ/mol. We also studied the effect of using different methods to calculate the charges of the inhibitor and different sizes of the perturbed group (the atoms that are described by soft-core potentials and are allowed to have differing coordinates)...
March 13, 2018: Journal of Computer-aided Molecular Design
Barbara Birk, Alexander Stähle, Mathias Meier, Markus Palm, Dorothee Funk-Weyer, Gerhard Breves, Harald Seulberger
The approving agencies for plant protection agents request xenobiotic metabolism and residue studies in rats, farm animals and plants (e.g. EU regulation 1107/2009) according to OECD guidelines. The specific intestinal physiology of ruminants might lead to specific residues, which should be investigated very carefully. Specific aspects of xenobiotic metabolism in ruminants may arise, which are investigated by performing additional in vivo studies. The aim of the present work is to asses a modified rumen simulation system (RUSITEC) for such studies in vitro...
March 12, 2018: ALTEX
J Denis, M-P Ledoux, Y Nivoix, R Herbrecht
Triazoles compounds are first-line agents for the treatment of invasive fungal diseases. Isavuconazole is the most recent triazole compound, approved in 2015 by the FDA and the EMA to treat invasive aspergillosis and mucormycosis. We reviewed here the in vitro activity of isavuconazole against a vast spectrum of species. Isavuconazole MICs were evaluated using CLSI, EUCAST or Etest methods, with no significant differences between the technics. Low MIC50 and MIC90 (<1μg/mL) were described for isavuconazole against the majority of Candida spp...
March 10, 2018: Journal de Mycologie Médicale
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