(EN) A series of novel, macrocyclic polyether compounds. The macrocycles have a 21-membered ring, containing six oxygen atoms, and they have a carboxy group (or a salt thereof) directed towards the interior of the ring. Administration of the compounds of the invention to ruminant animals (e.g. cattle and sheep) modifies their digestive fermentation processes such that the volatile fatty acids produced in the rumen contain a higher proportion of propionates rather than acetates, thereby increasing the efficiency of feed utilization in said ruminant animals. Additionally, the compounds of the invention show antibacterial activity $i(in vitro) against certain gram-positive microorganisms.(FR) L'invention se rapporte à une série de nouveaux composés de polyéther macrocyclique. Les macrocycles comprennent un noyau à 21 éléments, contenant six atomes d'oxygène, et comprennent un groupe carboxy (ou un sel de celui-ci) orienté vers l'intérieur du noyau. L'administration des composés de l'invention à des ruminants (par exemple des bovins et des ovins) modifie les procédés de fermentation digestive de sorte que les acides gras volatils produits dans le rumen contiennent une proportion plus élevée de propionates que d'acétates, ce qui accroît l'efficacité de l'utilisation des aliments chez ces ruminants. En outre, les composés de l'invention présentent une activité antibactérienne $i(in vitro) contre certains micro-organismes à gram positif.
Synthesis and Antifungal Activity of 1,3,2-Benzodithiazole S-Oxides
作者:Larry L. Klein、Clinton M. Yeung、David E. Weissing、Paul A. Lartey、S. Ken Tanaka、Jacob J. Plattner、Darcy J. Mulford
DOI:10.1021/jm00031a005
日期:1994.3
antifungal activity against several strains of Candida is described. For the preparation of derivatives bearing aromatic substituents, a novel electrophilic aromatic thiolation reaction was utilized which produced substituted aromatic 1,2-dithiol intermediates. The reactions of nucleophiles with the parent heterocyclicsystem have led to an efficient transamidation process which allows for the direct production