Letteratura scientifica selezionata sul tema "Ansamacrolides"
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Articoli di riviste sul tema "Ansamacrolides":
ISOBE, M. "ChemInform Abstract: Ansamacrolides". ChemInform 22, n. 19 (23 agosto 2010): no. http://dx.doi.org/10.1002/chin.199119314.
Koyama, Yasuhito, Martin J. Lear, Fumihiko Yoshimura, Isao Ohashi, Tomoko Mashimo e Masahiro Hirama. "Efficient Construction of the Kedarcidin Chromophore Ansamacrolide". Organic Letters 7, n. 2 (gennaio 2005): 267–70. http://dx.doi.org/10.1021/ol0477374.
Yoshimura, Fumihiko, Shinji Kawata e Masahiro Hirama. "Synthetic study of kedarcidin chromophore: atropselective construction of the ansamacrolide". Tetrahedron Letters 40, n. 47 (novembre 1999): 8281–85. http://dx.doi.org/10.1016/s0040-4039(99)01744-x.
Tesi sul tema "Ansamacrolides":
Antraygues, Kévin. "Conception, synthèse et évaluation biologique de nouveaux ansamacrolides dans le traitement d'infections bactériennes". Electronic Thesis or Diss., Université de Lille (2022-....), 2022. http://www.theses.fr/2022ULILS027.
Antimicrobial resistance is a major public health issue nowadays and this will be even more true in the coming decades. Among the bacteria involved in this alarming phenomenon, Acinetobacter baumannii and Mycobacterium abscessus are both resistant to many antibiotics currently available on the market. Research and development of new antibiotics is therefore necessary to fight these pathogens.Rifabutin, a semi-synthetic macrocyle of the rifamycin class, has recently shown interesting in vitro activities against A. baumannii and M. abscessus, which then translated into in vivo efficacy. Rifabutin therefore seems to be promising to the fight against these bacteria, but the use of this antibiotic is currently limited. In order to treat an infection caused by A. baumannii, rifabutin requires to be injected by intravenous route, which is not so easy because of the low water solubility of the molecule. Concerning the treatment of M. abscessus infections, rifabutin, although effective in vivo, has moderate activity against this mycobacterium, which could lead to therapeutic escape.Therefore, the work presented in this thesis manuscript seeks to address the limitations of rifabutin mentioned above.In a first part, water-soluble prodrugs of rifabutin have been synthesized in order to allow an intravenous injection and thus fight effectively against A. baumannii infections. To achieve the release of rifabutin after enzymatic cleavage in plasma, an intramolecular cyclization strategy was employed. After evaluation of the compounds in plasma stability assays, structure-stability relationship studies were performed, leading to the identification of three promising prodrugs. Additional in vitro studies were then conducted such as the measurement of aqueous solubility and bacterial growth inhibition, and finally an in vivo pharmacokinetic study was performed to be able to select for a preclinical candidate.In a second part, analogues of rifabutin modified at the C25 position were synthesized to identify more potent compounds. Based on a parallel chemistry strategy, a large number of derivatives were rapidly obtained and then evaluated against M. abscessus in order to conduct structure-activity relationship studies
Capitoli di libri sul tema "Ansamacrolides":
Isobe, Minoru. "Ansamacrolides". In Recent Progress in the Chemical Synthesis of Antibiotics, 103–34. Berlin, Heidelberg: Springer Berlin Heidelberg, 1990. http://dx.doi.org/10.1007/978-3-642-75617-7_4.