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131.
Markus Leibeling Dennis C. Koester Martin Pawliczek Daniel Kratzert Birger Dittrich Daniel B. Werz 《Bioorganic & medicinal chemistry》2010,18(11):3656-3667
Herein we describe the synthesis of highly substituted chromans and isochromans using carbohydrates as starting materials. The key step of our synthetic approach is the annelation of the benzene moiety via a highly efficient Pd-catalyzed domino reaction. This powerful approach led to a small library of highly substituted chromans and isochromans by making use of a variety of different diynes and bromoglycals. We investigated several Pd-catalysts in order to improve the yields and to enlarge the scope of the domino reaction. Furthermore, we elucidated the mechanistic picture of the reaction with isotope-labelling experiments. Most probably the reaction proceeds via an oxidative addition followed by two carbopalladation steps and a final cyclization reaction. 相似文献
132.
Nantermet PG Burgey CS Robinson KA Pellicore JM Newton CL Deng JZ Selnick HG Lewis SD Lucas BJ Krueger JA Miller-Stein C White RB Wong B McMasters DR Wallace AA Lynch JJ Yan Y Chen Z Kuo L Gardell SJ Shafer JA Vacca JP Lyle TA 《Bioorganic & medicinal chemistry letters》2005,15(11):2771-2775
In this study, we have demonstrated that the critical hydrogen bonding motif of the established 3-aminopyrazinone thrombin inhibitors can be effectively mimicked by a 2-aminopyridine N-oxide. As this peptidomimetic core is more resistant toward oxidative metabolism, it also overcomes the metabolic liability associated with the pyrazinones. An optimization study of the P(1) benzylamide delivered the potent thrombin inhibitor 21 (K(i) = 3.2 nM, 2xaPTT = 360 nM), which exhibited good plasma levels and half-life after oral dosing in the dog (C(max) = 2.6 microM, t(1/2) = 4.5 h). 相似文献
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134.
ABSTRACT For seabirds raising young under conditions of limited food availability, reducing chick provisioning and chick growth rates are the primary means available to avoid abandonment of a breeding effort. For most seabirds, however, baseline data characterizing chick growth and development under known feeding conditions are unavailable, so it is difficult to evaluate chick nutritional status as it relates to foraging conditions near breeding colonies. To address this need, we examined the growth and development of young Caspian Terns (Hydroprogne caspia), a cosmopolitan, generalist piscivore, reared in captivity and fed ad libitum and restricted (ca. one‐third lower caloric intake) diets. Ad libitum‐fed chicks grew at similar rates and achieved a similar size at fledging as previously documented for chicks in the wild and had energetic demands that closely matched allometric predictions. We identified three general characteristics of food‐restricted Caspian Tern chicks compared to ad libitum chicks: (1) lower age‐specific body mass, (2) lower age‐specific skeletal and feather size, such as wing chord length, and (3) heightened levels of corticosterone in blood, both for baseline levels and in response to acute stress. Effects of diet restriction on feather growth (10–11% slower growth in diet‐restricted chicks) were less pronounced than effects on structural growth (37–52% slower growth) and body mass (24% lower at fledging age), apparently due to preferential allocation of food resources to maintain plumage growth. Our results suggest that measurements of chick body mass and feather development (e.g., wing chord or primary length) or measurement of corticosterone levels in the blood would allow useful evaluation of the nutritional status of chicks reared in the wild and of food availability in the foraging range of adults. Such evaluations could also inform demography studies (e.g., predict future recruitment) and assist in evaluating designated piscivorous waterbird conservation (colony) sites. 相似文献
135.
Craig Byron Hawley Kunz Heather Matuszek Stephanie Lewis Daniel Van Valkinburgh 《Journal of morphology》2011,272(2):230-240
We use an outbred laboratory mouse strain (ICR/CD‐1, Charles River Laboratories, Inc.) to model a type of preprimate locomotion associated with rudimentary pedal grasping. Ten male mice were assigned to either control or climbing groups (n = 5 per group). Climbing mice lived within a specialized terrarium that included ~7.5 m of thin branches (5 and 10 cm long) with a thickness of 3.3mm, arranged in a reticulated canopy. Food, water, and a nest site were placed among the branches. To discourage mice from palmigrade or digitigrade locomotion, the floor of the terrarium was flooded with a few centimeters of water. Climbing mice were placed in this setting upon weaning and reared for 3 months until they were mature in size. Litter, and age‐matched controls were also maintained for comparison with climbers. Climbing mice quickly acclimated to the requirements of the fine‐branch model using the foot and tail for grasping and balance. At maturity, climbing and control mice exhibited minor, but significant, morphological plasticity. For climbers, this includes a greater angle of the femoral neck, larger patellar groove index, relatively shorter talar neck length, and more circular talar head aspect ratio (P < 0.10). Climbers also exhibit increased curvature of the distal third metacarpal, decreased talar head angle, and relatively longer caudal vertebrae transverse processes (P < 0.05). These results in a small‐bodied eutherian mammal suggest that facultative hallucial opposability and coordinated tail use enable a kind of grasping active arboreal quadrupedality relevant to the latest stages of pre‐euarchontan evolution. In light of these data, we hypothesize that a unique advantage of mouse‐sized mammals is that they exhibit a highly flexible body plan allowing them to engage in a diverse array of anatomical positions without requiring specific limb morphologies. J. Morphol.,2011. © 2010 Wiley‐Liss, Inc. 相似文献
136.
137.
Useful Species Richness, Proportion of Exotic Species, and Market Orientation on Amazonian Dark Earths and Oxisols Anthropogenic soils of Amazonia, known as Amazonian Dark Earths (ADE), are environments with elevated soil fertility that can produce crops that otherwise yield poorly on the leached and highly acidic Oxisols that dominate much of the basin. While ADE sites near urban centers often attract commercial horticultural production of nutrient–demanding exotics, these soils are also considered possibly unique reservoirs of endemic agrobiodiversity because of their relationship to pre–Columbian indigenous occupation. Through botanical surveys and interviews with smallholder farmers, this study compared useful species richness, proportion of exotic species, and market orientation of farms situated on ADE and non–anthropogenic Oxisols in the municipality of Borba in Central Brazilian Amazonia. Species richness was similar on Amazonian Dark Earth and Oxisol farms (19.6 spp vs. 18.3 spp); however, ADE farms showed significantly higher proportions of exotic species (39% vs. 26%; p = 0.025). Furthermore, ADE farms in Borba demonstrated significantly higher market orientation (61.0% vs. 47.3%; p = 0.028), likely a result of the advantage of Amazonian Dark Earths for production of crops that are nutrient–demanding or pH–sensitive crops that have higher values in the nearby regional market of Manaus. 相似文献
138.
The direct visualization of subcellular dynamic processes is often hampered by limitations in the resolving power achievable with conventional microscopy techniques. Fluorescence recovery after photobleaching has emerged as a highly informative approach to address this challenge, permitting the quantitative measurement of the movement of small organelles and proteins in living functioning cells, and offering detailed insights into fundamental cellular phenomena of physiological importance. In recent years, its implementation has benefited from the increasing availability of confocal microscopy systems and of powerful labeling techniques based on genetically encoded fluorescent proteins or other chemical markers. In this review, we present fluorescence recovery after photobleaching and related techniques in the context of contemporary neurobiological research and discuss quantitative and semi‐quantitative approaches to their interpretation. 相似文献
139.
Rachel D. Neuenhoff Daniel F. Cowan Heidi Whitehead Christopher D. Marshall 《Marine Mammal Science》2011,27(1):195-216
Compilation of marine mammal demographic data is central to management efforts. However, marine mammal length‐at‐age growth curves demonstrate limitations. Physiological growth parameters of terrestrial mammals are typically estimated using curvilinear models fit to size‐at‐age data along a time series from conception to senescence. The difficulty of collecting and aging prenatal cetaceans is addressed here, and growth parameters of common bottlenose dolphins (Tursiops truncatus) along coastal Texas were estimated using length‐at‐age information from a broader scope of age classes, including late‐term fetuses. A Gompertz growth curve fit to pre‐ and postnatal data underestimated size parameters, but demonstrated similar growth rate constants (k) to an exclusively postnatal model. However, when growth parameters were broken out, the absolute growth rate (G) and rate of growth decay (g) decreased (0.44 from 0.27 and 0.55 from 0.39, respectively), which underscores the importance of reporting k in its expanded form (G/g). Although the Gompertz fits most age classes well, it cannot explain growth in all age classes. We argue that a novel sigmoidal model would be more useful for inference. 相似文献
140.
Daniel R. Vining Jr. 《Evolution and human behavior》2011,32(5):364-367
This article looks at two articles recently published here, one by R. Hopcroft [“Sex, status, and reproductive success in the contemporary United States,” Evolution and Human Behavior 27 (2006) 104–120] the second by M. Fieder and S. Huber [“The effects of sex and childlessness on reproductive effort in modern humans,” Evolution and Human Behavior 28 (2007) 392–398]. They both report a positive relationship between male income and male fertility, which marks a real advancement in our knowledge. Hopcroft speculates at the end of her article that the father's status and female fertility will be positive, too. At this point, this will depend on her and others' reaction to the efforts of S. Huber, F. Bookstein, and M. Fiedler. (2010). Socioeconomic status, education, and reproduction in modern women: an evolutionary perspective. American Journal of Human Biology, 22, 578-587. M. Fieder and S. Huber. (2007). The effects of sex and childlessness on the association between status and reproductive output in modern society. Evolution and Human Behavior, 2, 392-398. are not explicit about this relationship; their closing lines just leave open the possibility that it might be positive. The conclusion is that sociobiology is not really relevant yet to the understanding of modern, industrial society, urban civilization in general, except to show us the various restraints imposed by inborn human nature. 相似文献