76029-50-0Relevant articles and documents
A New Dioxazolone for the Synthesis of 1,2-Aminoalcohols via Iridium(III)-Catalyzed C(sp3)?H Amidation
Antien, Kevin,Geraci, Andrea,Parmentier, Michael,Baudoin, Olivier
supporting information, p. 22948 - 22955 (2021/09/09)
Vicinal aminoalcohols are widespread structural motifs in bioactive molecules. We report the development of a new dioxazolone reagent containing a p-nitrophenyldifluoromethyl group, which 1. displays a good safety profile; 2. shows a remarkably high react
Oxime glucokinase activators
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Page/Page column 7, (2008/12/06)
Disclosed herein are pyrazole glucokinase activators of the formula (I): that are useful for the treatment of metabolic diseases and disorders.
Studies on anti-MRSA parenteral cephalosporins II. Synthesis and antibacterial activity of 7 β-[2-(5-Amino-1,2,4-thiadiazol-3-yl)- 2(Z)-alkoxyiminoacetamido]-3(substituted imidazo[1,2-b] pyridazinium-1-yl)methyl-3-cephem-4-carboxylates and related compounds
Ishikawa,Kamiyama,Matsunaga,Tawada,Iizawa,Okonogi,Miyake
, p. 1071 - 1085 (2007/10/03)
In an effort to discover a novel cefozopran (CZOP) derivative having excellent antibacterial activity against methicillin-resistant Staphylococcus aureus (MRSA), we performed chemical modification of the alkoxyimino moiety and imidazo[1,2-b]pyridazinium group of CZOP. Among the prepared compounds, the cyclopentyloxyimino derivative 7β-[2-(5- amino-1,2, 4-thiadiazol-3-yl)-2(Z) -cyclopentyloxyiminoacetamido] -3-(3,6-diaminoimidazo[1,2- b]pyridazinium-1-yl)methyl-3-cephem-4-carboxylate (20g) showed the most potent anti-MRSA activity, reflecting its high affinity (IC50=1.6μg/ml) for penicillin binding protein 2' (PBP2'), although its anti-MRSA activity was slightly inferior to that of vancomycin (VCM). In experimental systemic infection in mice, however, 20g showed activity comparable to that of VCM against MRSA. In addition, 20g showed activity similar or slightly inferior to that of CZOP against Pseudomonas aeruginosa both in vitro and in vivo. Considering its favorable antibacterial activity profile, 20g was considered to be the most promising CZOP derivative for further studies.