SUMMARYDeuterium exchange labelling using [Ir(COD)(Cy3P)(Py)]PFg as catalyst and deuterium gas was studied on a number of substituted acetanilides. In most cases products containing deuterium ortlio to the anilide group were obtained with a high degree of enrichment. With one exception no evidence for nietn, p r n or anilide methyl labelling was seen. The catalyst was also effective in the ortlia deuteration of acetophenone, benzophenone and the P-lactam containing compound Sch 48461.
3-Guanidinopropionic acid (1, PNU-10483) has been demonstrated to both improve insulin sensitivity and to promote weight loss selectively from adipose tissue in animal models of non-insulin-dependent diabetes mellitus (NIDDM). However, 1 has also been shown to be a substrate for both the creatine transporter and creatine kinase, leading to marked accumulation in muscle tissue as the corresponding N-phosphate 4. In an effort to identify novel entities that maintain antidiabetic potency without susceptibility to creatine-like metabolism, an analogue program was undertaken to explore the effects of various structural modifications, including homologation, simple substitution, single atom mutations, and bioisosteric replacements for the guanidine and carboxylic acid. Overall, the scope of activity encompassed by the set of new analogues proved to be exceedingly narrow. Notable exceptions demonstrating equivalent or improved antidiabetic activity included the alpha-amino derivative 29, aminopyridine 47, isothiourea 67, and aminoguanidine 69. On the basis of its superior therapeutic ratio, aminoguanidine 69 was selected for preclinical development and became the foundation for a second phase of analogue work. Furthermore, in vitro studies demonstrated that 69 is markedly less susceptible to phosphorylation by creatine kinase than the lead 1, suggesting that it should have less potential for accumulation in muscle tissue than 1.
The purpose of this study was to examine the relationship between mathematics content knowledge and teacher efficacy during an elementary mathematics methods course. A positive moderate relationship between content knowledge and personal teaching efficacy was found, and this relationship was stable during the course. No relationship was found between content knowledge and outcome expectancy. Written artifacts were used to understand and elaborate on these findings. Those data suggest that prior learning experiences may help explain this relationship. Additionally, they suggest that preservice teachers with different levels of content knowledge may attend to different sources of information when making efficacy judgments about teaching.
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