A New Bactericidal Lead Structure for the Protection of Materials.

Abstract

A New Bactericidal Lead Structure for the Protection of Materials. -(I) shows strong antibacterial activity down to levels of below 100ppm but increases the number of mutations in Ames tests. An improved synthesis of (I) is given. -(VOGL*, E.; BRUNS, R.; KRETSCHIK, O.; UHR, H.; KAULEN, J.; KUGLER, M.; WACHTLER, P.; KREISS, W.; EBERZ, G.; Bioorg. Med. Chem. Lett. 15 (2005) 3, 625-629; Mater. Prot. Prod., Bayer AG, D-51368 Leverkusen, Germany; Eng.) -M. Bohle 25-127

Synthesis and properties of vicinal cyanoximes of adamantane series

“…Examples are known of applying β-cyanoximes in the preparation of 5-aminoisoxazoles [1,2], including the condensed ones [3], and also the derivatives of indole [4], azarine [5], 5-amino-1,3-oxazole, pyrrolidinone, and oxazolo [5,4-b]pyridine [6]. Usually the cyanoximes are obtained from ketonitriles [4,7,8] or enaminonitriles [1] and hydroxylamine, and also by reduction of β-nitrocyanides [9].…”

Chemoselective Reduction of Functionalized 5-Nitroisoxazoles: Synthesis of 5-Amino- and 5-[Hydroxy(tetrahydrofuran-2-yl)amino]isoxazoles

“…The significant interest in isoxazole derivatives stems from their versatility as synthetic building blocks and their application in various fields such as agriculture, industry, and medicine. 1 In particular, aminoisoxazoles are known to possess a wide range of physiological activities, for example, cytotoxic (anticancer), 2 biocidal, 3 anti-inflammatory and immune-suppressive 4 activities. Aminosubstituted isoxazoles are also employed in the preparation of fused heterocyclic systems, such as isoxazolopyridines, isoxazolopyrimidines, and isoxazolodiazepines, which represent valuable scaffolds in pharmacological agents.…”