- Antimicrobial and KPC/AmpC inhibitory activity of functionalized benzosiloxaboroles
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A series of 22 benzosiloxaboroles, silicon analogues of strong antimicrobial agents - benzoxaboroles, have been synthesized and tested against β-lactamases KPC- and pAmpC-producing strains of Gram-negative rods. Comprehensive structural-property relationship studies supported by molecular modelling as well as biological studies reveal that 6-B(OH)2-substituted derivative 27 strongly inhibits the activity of cephalosporinases (chromosomally encoded AmpC and plasmid encoded CMY-2) and KPC carbapenemases. It also shows strong ability to inhibit growth of the strains producing KPC-3 when combined with meropenem. In addition, halogen-substituted (mono-, di- or tetra-) benzosiloxaboroles demonstrate high antifungal activity (MIC 1.56–6.25 mg/L) against C. tropicalis, C. guilliermondii and S. cerevisiae. The highest activity against pathogenic yeasts (C. albicans, C. krusei and C. parapsilosis - MICs 12.5 mg/L) and against Gram-positive cocci (S. aureus and E. faecalis - 6.25 mg/L and 25 mg/L respectively) was displayed by 6,7-dichloro-substituted benzosiloxaborole. The studied systems exhibit low cytotoxity toward human lung fibroblasts.
- Durka, Krzysztof,Laudy, Agnieszka E.,Charzewski, ?ukasz,Urban, Mateusz,St?pień, Karolina,Tyski, Stefan,Krzy?ko, Krystiana A.,Luliński, Sergiusz
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- Ruthenium-Catalyzed Cycloisomerization of 2,2′-Diethynyl- biphenyls Involving Cleavage of a Carbon-Carbon Triple Bond
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A ruthenium complex catalyzes a new cycloisomerization reaction of 2,2′-diethynylbiphenyls to form 9-ethynylphenanthrenes, thereby cleaving the carbon-carbon triple bond of the original ethynyl group. A metal-vinylidene complex is generated from one of th
- Matsuda, Takanori,Kato, Kotaro,Goya, Tsuyoshi,Shimada, Shingo,Murakami, Masahiro
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supporting information
p. 1941 - 1943
(2016/02/14)
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