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Research on the correlation between the Pummerer reaction mechanism and β-lactam formation during penicillin biosynthesis is discussed based on our silicon-induced asymmetric Pummerer type reaction.
Two monobactam derivatives, potassium (3Z)-((N-methyl-1,2,3-triazol-4-yl)methylene)-4-phenylthio-2-azetidinone-1-sulfonate and potassium (3 E )-((N-methyl-1,2,3-triazol-4-yl)methylene)-4-(1,2,3-triazol-1-yl)-2-azetidinone-1-sulfonate, were synthesized and tested for β-lactamase inhibitory activity.
7-Silyl- and 7-germylcephalosporanates in the form of a mixture of 7a and 7b stereoisomers were prepared by the interaction of hydrosilanes and a hydrogermane * with sulfones of tert-butyl esters of 7-diazocephalosporanic acid and 7-diazodesacetoxycephalosporanic acid in the presence of rhodium...
A new series of 2-spiro(2′,2′-diphenylcyclopropane) cephalosporin sulfones was synthesizes as potent human leukocyte elastase inhibitors.
By the interaction of heterocyclic thiols with sulfoxides of 6,6-dihydro- and 6α-chloropenicillanates, derivatives of 4-heteryldithio-2-azetidinones have been synthesized, as well as products of their cyclization to form 2β-heterylthiomethyl-and 2β-halomethyl-substituted penicillanates and an...
Optimization of the antibacterial activity of 4-amino trinem, obtained through chemical modification of the basicity of the amino group at position 4, has led to the identification of a very interesting compound characterized by a broad spectrum of activity including Pseudomonas aeruginosa .
Starting from 3,5-dimethylisoxazole the carboxylic acids I and V, the amino acids VIII (L-) and IX (D-), and the ureido acids X (L-) and XI (D-) were prepared, which were used for the synthesis of the new cephalosporins XVIIb, XXa-c (L-), and XXIb (D-). The in vitro antibacterial activity of...
A series of 7α-methoxy-2-((substituted)methylene)cephem sulfones was synthesized. The compounds with an acetoxy group at the C-3′ position as a leaving group were found to be potent inhibitors of HLE. Selected compounds are also found to be antithrombin agents.
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