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      Synthesis and antibacterial activity of some 5,5'-(1,4-phenylene)-bis-1,3,4-oxadiazole and bis-1,2,4-triazole derivatives as precursors of new S-nucleosides

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          Abstract

          Five compounds, namely 5,5'-benzene-1,4-diylbis(1,3,4-oxadiazole-2-thiol)6 and 5,5'-benzene-1,4-diylbis(1H-1,2,4-triazole-3-thiol) 7a and its derivatives 7b-d were synthesized. Two related S-nucleosides 9 and 10 have been prepared from 6 and 7a Some of these synthesized compounds were tested in vitro by spotting on Mueller Hinton Agar medium against some Gram-positive bacteria, Staphylococcus aureus and Enterococcus faecalis and three Gram-negative bacteria Escherichia coli, Pseudomonasaeruginosa, Pseudomonas fluorescens and compared with the known antibiotics cephalosporin (cefotaxim) and gentamycin. Compound 6: showed significant inhibitory activity against Gram-positive E. faecalis and Gram-negative E. coli bacteria while the others have shown variable inhibition activity.

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          Methods for Dilution Antimicrobial Susceptibility Tests for Bacteria that Grow Aerobically

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            Inside HDAC with HDAC inhibitors.

            Histone deacetylase inhibitors are a large group of diverse molecules intrinsically able to inhibit cell proliferation in various cancer cell lines. Their apoptotic effects have been linked to the modulation in the expression of several regulatory tumor suppressor genes caused by the modified status of histone acetylation, a key event in chromatin remodelling. As the initial histone deacetylase activity of HDAC has been extended to other proteins, the possible other biological mechanisms modified by HDAC inhibitor treatments are still to be clarified. The need for HDAC isoform selective inhibitors is an important issue to serve this goal. This review discusses the approaches proposed by several research groups working on the synthesis of HDAC inhibitors, based on modelling studies and the way these findings were used to obtain new HDAC inhibitors with possible isoform selectivity. Copyright (c) 2010 Elsevier Masson SAS. All rights reserved.
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              Bithiopheneimide-dithienosilole/dithienogermole copolymers for efficient solar cells: information from structure-property-device performance correlations and comparison to thieno[3,4-c]pyrrole-4,6-dione analogues.

              Rational creation of polymeric semiconductors from novel building blocks is critical to polymer solar cell (PSC) development. We report a new series of bithiopheneimide-based donor-acceptor copolymers for bulk-heterojunction (BHJ) PSCs. The bithiopheneimide electron-deficiency compresses polymer bandgaps and lowers the HOMOs--essential to maximize power conversion efficiency (PCE). While the dithiophene bridge progression R(2)Si→R(2)Ge minimally impacts bandgaps, it substantially alters the HOMO energies. Furthermore, imide N-substituent variation has negligible impact on polymer opto-electrical properties, but greatly affects solubility and microstructure. Grazing incidence wide-angle X-ray scattering (GIWAXS) indicates that branched N-alkyl substituents increased polymer π-π spacings vs linear N-alkyl substituents, and the dithienosilole-based PBTISi series exhibits more ordered packing than the dithienogermole-based PBTIGe analogues. Further insights into structure-property-device performance correlations are provided by a thieno[3,4-c]pyrrole-4,6-dione (TPD)-dithienosilole copolymer PTPDSi. DFT computation and optical spectroscopy show that the TPD-based polymers achieve greater subunit-subunit coplanarity via intramolecular (thienyl)S···O(carbonyl) interactions, and GIWAXS indicates that PBTISi-C8 has lower lamellar ordering, but closer π-π spacing than does the TPD-based analogue. Inverted BHJ solar cells using bithiopheneimide-based polymer as donor and PC(71)BM as acceptor exhibit promising device performance with PCEs up to 6.41% and V(oc) > 0.80 V. In analogous cells, the TPD analogue exhibits 0.08 V higher V(oc) with an enhanced PCE of 6.83%, mainly attributable to the lower-lying HOMO induced by the higher imide group density. These results demonstrate the potential of BTI-based polymers for high-performance solar cells, and provide generalizable insights into structure-property relationships in TPD, BTI, and related polymer semiconductors.
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                Author and article information

                Contributors
                Role: ND
                Role: ND
                Role: ND
                Journal
                sajc
                South African Journal of Chemistry
                S.Afr.j.chem. (Online)
                The South African Chemical Institute (Durban )
                1996-840X
                2012
                : 65
                : 0
                : 30-35
                Affiliations
                [1 ] University of Sciences and Technology-Mohamed Boudiaf-Oran-USTO Algeria
                [2 ] Université Verlaine France
                Article
                S0379-43502012000100006
                5820896e-675a-4bcf-8955-571e86a9299c

                http://creativecommons.org/licenses/by/4.0/

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                SciELO South Africa

                Self URI (journal page): http://www.scielo.org.za/scielo.php?script=sci_serial&pid=0379-4350&lng=en
                Categories
                Chemistry, Analytical
                Chemistry, Applied
                Chemistry, Inorganic & Nuclear
                Chemistry, Medicinal
                Chemistry, Multidisciplinary
                Chemistry, Organic
                Chemistry, Physical
                Electrochemistry

                Electrochemistry,Clinical chemistry,Organic & Biomolecular chemistry,Physical chemistry,Analytical chemistry,General chemistry,Industrial chemistry,Inorganic & Bioinorganic chemistry
                Terephthalic acid,antimicrobial activity,S-nucleosides,1H-1,2,4-triazole,1,3,4-oxadiazole

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