216487-29-5Relevant articles and documents
USE OF NITROOXY ORGANIC MOLECULES IN FEED FOR REDUCING METHANE EMISSION IN RUMINANTS, AND/OR TO IMPROVE RUMINANT PERFORMANCE
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Paragraph 0115; 0116, (2014/06/11)
The present invention relates to a method for reducing the production of methane emanating from the digestive activities of a ruminant and/or for improving ruminant animal performance by using, as active compound at least one organic molecule substituted at any position with at least one nitrooxy group, or a salt thereof, which is administrated to the animal together with the feed. The invention also relates to the use of these compounds in feed and feed additives such as premix, concentrates and total mixed ration (TMR) or in the form of a bolus.
2-Alkynyl-8-aryladenines possessing an amide moiety: Their synthesis and structure-activity relationships of effects on hepatic glucose production induced via agonism of the A2B adenosine receptor
Harada,Asano,Kawata,Inoue,Horizoe,Yasuda,Nagata,Murakami,Nagaoka,Kobayashi,Tanaka,Abe
, p. 2709 - 2726 (2007/10/03)
A series of 2-alkynyl-8-aryladenine derivatives bearing an amide moiety at the 9-position of adenine was synthesized. These analogues were evaluated for inhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytes. The m-primary benzamide derivative 15f was the most potent compound (IC50 = 0.017 μM), being 15-fold more active than the corresponding 9-methyl derivative (1). Compound 15f showed 72- and 5.2-fold selectivity for human A2B receptor versus human A1 and A2A receptors, respectively. Structure-activity relationship (SAR) studies of the synthesized compounds indicated that a three-carbon linker, fixed in the form of a benzene ring, between the adenine core and the amide moiety is important for both A2B antagonistic activity and selectivity. The IC50 values in rat hepatocyte glucose assay correlated well with the IC50 values in cAMP assay using Chinese hamster ovary cells stably transfected with human A2B receptors (r2 = 0.94). The A1 and A2A affinities showed no correlation with the potency to inhibit NECA-induced glucose production. These results strongly support our previous conclusion that adenosine agonist-induced hepatic glucose production in rat hepatocytes is mediated through the A2B receptor.
Novel antiarthritic agents with 1,2-isothiazolidine-1-,1-dioxide (γ- sultam) skeleton: Cytokine suppressive dual inhibitors of cyclooxygenase-2 and 5-lipoxygenase
Inagaki, Masanao,Tsuri, Tatsuo,Jyoyama, Hirokuni,Ono, Takashi,Yamada, Katsutoshi,Kobayashi, Mika,Hori, Yozo,Arimura, Akinori,Yasui, Kiyoshi,Ohno, Kouji,Kakudo, Shinji,Koizumi, Kenzo,Suzuki, Ryuji,Kato, Miyako,Kawai, Shinichi,Matsumoto, Saichi
, p. 2040 - 2048 (2007/10/03)
Various 1,2-isothiazolidine-1,1-dioxide (γ-sultam) derivatives containing an antioxidant moiety, 2,6-di-tert-butylphenol substituent, were prepared. Some compounds, which have a lower alkyl group at the 2-position of the γ-sultam skeleton, showed potent i