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191.
Lucie Emilie Schmaltz Cédric Juillet Joost Marius Tinbergen Yvonne Ingje Verkuil Joslyn Corstiaan Elbert Wouter Hooijmeijer Theunis Piersma 《Population Ecology》2015,57(4):613-624
The ruff Philomachus pugnax, a lekking shorebird wintering in Africa and breeding across northern Eurasia, declined severely in its western range. Based on a capture-mark-resighting programme (2004–2011) in the westernmost staging area in Friesland (the Netherlands), we investigated changes in apparent annual survival in relation to age and sex to explore potential causes of decline. We also related temporal variation in apparent survival to environmental factors. We used the Capture-Mark-Recapture multievent statistical framework to overcome biases in survival estimates after testing for hidden heterogeneity of detection. This enabled the estimation of the probability to belong to high or low detectability classes. Apparent survival varied between years but was not related to weather patterns along the flyway, or to flood levels in the Sahel. Over time, a decline in apparent survival is suggested. Due to a short data series and flag loss in the last period this cannot be verified. Nevertheless, the patterns in sex-specific detectability and survival lead to new biological insights. Among highly detectable birds, supposedly most reliant on Friesland, males survived better than females ( = 0.74, range 0.51–0.93; = 0.51, range 0.24–0.81). Among low detectable birds, the pattern is reversed ( = 0.64, range 0.37–0.89; = 0.73, range 0.48–0.93). Probably the staging population contains a mixture of sex-specific migration strategies. A loss of staging females could greatly affect the dynamics of the western ruff population. Further unravelling of these population processes requires geographically extended demographic monitoring and the use of tracking devices. 相似文献
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Jamieson C Maclean JK Brown CI Campbell RA Gillen KJ Gillespie J Kazemier B Kiczun M Lamont Y Lyons AJ Moir EM Morrow JA Pantling J Rankovic Z Smith L 《Bioorganic & medicinal chemistry letters》2011,21(2):805-811
Starting from compound 1, we utilized biostructural data to successfully evolve an existing series into a new chemotype with a promising overall profile, exemplified by 19. 相似文献
197.
De Savi C Pape A Sawyer Y Milne D Davies C Cumming JG Ting A Lamont S Smith PD Tart J Page K Moore P 《Bioorganic & medicinal chemistry letters》2011,21(11):3301-3306
A new achiral class of N-hydroxyformamide inhibitor of both ADAM-TS4 and ADAM-TS5, 2 has been discovered through modification of the complex P1 group present in historical inhibitors 1. This structural change improved the DMPK properties and greatly simplified the synthesis whilst maintaining excellent cross-MMP selectivity profiles. Investigation of structure-activity and structure-property relationships in the P1 group resulted in both ADAM-TS4 selective and mixed ADAM-TS4/5 inhibitors. This led to the identification of a pre-clinical candidate with excellent bioavailability across three species and predicting once daily dosing kinetics. 相似文献
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Zhang YK Plattner JJ Freund YR Easom EE Zhou Y Gut J Rosenthal PJ Waterson D Gamo FJ Angulo-Barturen I Ge M Li Z Li L Jian Y Cui H Wang H Yang J 《Bioorganic & medicinal chemistry letters》2011,21(2):644-651
A series of boron-containing benzoxaborole compounds was designed and synthesized for a structure-activity relationship investigation surrounding 7-(HOOCCH2CH2)-1,3-dihydro-1-hydroxy-2,1-benzoxaborole (1) with the goal of discovering a new antimalarial treatment. Compound 1 demonstrates the best potency (IC50 = 26 nM) against Plasmodium falciparum and has good drug-like properties, with low molecular weight (206.00), low ClogP (0.86) and high water solubility (750 μg/mL at pH 7). 相似文献
199.
Sexton KE Barrett S Bridgwood K Carroll M Dettling D Du D Fakhoury S Fedij V Hu LY Kostlan C Pocalyko D Raheja N Smith Y Shanmugasundaram V Wade K 《Bioorganic & medicinal chemistry letters》2011,21(18):5230-5233
A series of pantolactam based compounds were identified as potent antagonists for the androgen receptor (AR). Those that possessed properties suitable for topical delivery were evaluated in the validated Hamster Ear Model. Several compounds were found to be efficacious in reducing wax esters, a major component of sebum, initiating further preclinical work on these compounds. 相似文献
200.
Bordon Y 《Nature reviews. Immunology》2011,11(5):300-301