ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTStructure of pyrrolosine: a novel inhibitor of RNA synthesis, from the actinomycete Streptomyces albusSusumu Ikegami, Haruhiko Isomura, Noboru Tsuchimori, Yasuko T. Osano, Tetsuro Hayase, Tomoko Yugami, Haruyuki Ohkishi, and Takao MatsuzakiCite this: J. Am. Chem. Soc. 1990, 112, 26, 9668–9669Publication Date (Print):December 1, 1990Publication History Published online1 May 2002Published inissue 1 December 1990https://pubs.acs.org/doi/10.1021/ja00182a052https://doi.org/10.1021/ja00182a052research-articleACS PublicationsRequest reuse permissionsArticle Views161Altmetric-Citations17LEARN ABOUT THESE METRICSArticle Views are the COUNTER-compliant sum of full text article downloads since November 2008 (both PDF and HTML) across all institutions and individuals. These metrics are regularly updated to reflect usage leading up to the last few days.Citations are the number of other articles citing this article, calculated by Crossref and updated daily. Find more information about Crossref citation counts.The Altmetric Attention Score is a quantitative measure of the attention that a research article has received online. Clicking on the donut icon will load a page at altmetric.com with additional details about the score and the social media presence for the given article. Find more information on the Altmetric Attention Score and how the score is calculated. Share Add toView InAdd Full Text with ReferenceAdd Description ExportRISCitationCitation and abstractCitation and referencesMore Options Share onFacebookTwitterWechatLinked InRedditEmail Other access optionsGet e-AlertscloseSupporting Info (1)»Supporting Information Supporting Information Get e-Alerts
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ABSTRACT TAK-456 is a novel oral triazole compound with potent and broad-spectrum in vitro antifungal activity and strong in vivo efficacy against Candida albicans and Aspergillus fumigatus . TAK-456 inhibited sterol synthesis of C. albicans and A. fumigatus by 50% at 3 to 11 ng/ml. TAK-456 showed strong in vitro activity against clinical isolates of Candida spp., Aspergillus spp., and Cryptococcus neoformans , except for Candida glabrata . The MICs at which 90% of the isolates tested were inhibited byTAK-456, fluconazole, itraconazole, voriconazole, and amphotericin B were 0.25, 4, 0.5, 0.13, and 0.5 μg/ml, respectively, for clinical isolates of C. albicans and 1, >64, 0.5, 0.5, and 0.5 μg/ml, respectively, for clinical isolates of A. fumigatus . Therapeutic activities of TAK-456 and reference triazoles against systemic lethal infections caused by C. albicans and A. fumigatus in mice were investigated by orally administering drugs once daily for 5 days, and efficacies of the compounds were evaluated by the prolongation of survival. In normal mice, TAK-456 and fluconazole were effective against infection caused by fluconazole-susceptible C. albicans at a dose of 1 mg/kg. In transiently neutropenic mice, therapeutic activity of TAK-456 at 1 mg/kg of body weight against infection with the same strain was stronger than those at 1 mg/kg of fluconazole. TAK-456 was effective against infections with two strains of fluconazole-resistant C. albicans at a dose of 10 mg/kg. TAK-456 also expressed activities similar to or higher than those of itraconazole against the infections caused by two strains of A. fumigatus in neutropenic mice at a dose of 10 mg/kg. These results suggest that TAK-456 is a promising candidate for development for the treatment of candidiasis and aspergillosis in humans.
An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available from the CCDC and typically includes 3D coordinates, cell parameters, space group, experimental conditions and quality measures.
The therapeutic activity of cefozopran, a new semisynthetic parenteral cephalosporin, was compared with those of ceftazidime, ampicillin, imipenem/cilastatin and ofloxacin against an ascending mixed urinary tract infection induced in mice with Enterococcus faecalis TN2005 and Pseudomonas aeruginosa P9. Cefozopran significantly reduced viable cell counts of both organisms in the kidneys. Ceftazidime, imipenem/cilastatin and ofloxacin were active against only P. aeruginosa, and ampicillin was active against only E. faecalis.
Abstract External application of 50 μg ml-1 adenosine inhibits development of the starfish Asterina pectinifera at the 256-cell stage when all the embryonic cells differentiate to epithelial cells. Intracellular concentration of adenosine in the adenosine-treated embryo is 2·7 times higher than those of the normal embryo whereas the contents of ATP, ADP, AMP and adenosine 3′,5′-monophosphate are the same for both embryos. Adenosine causes more than 95 % reduction in the rate of protein, DNA and RNA syntheses. By returning the embryo to normal sea water, macromolecular synthesis restarts and the embryo develops to the bipin-naria stage.
An inhibitor of development of the starfish Asterina pectinifera was purified to homogeneity from a culture of the bacterium Bacillus subtilis , and was identified as adenosine. Adenosine at 6 μg/ml was shown to halt embryonic development specifically at the 256‐cell stage when all the embryonic cells differentiate into epithelial cells. By returning treated embryos to normal seawater, they developed normally to the bipinnaria stage.
