A new 1 km global IIASA-IFPRI cropland percentage map for the baseline year 2005 has been developed which integrates a number of individual cropland maps at global to regional to national scales. The individual map products include existing global land cover maps such as GlobCover 2005 and MODIS v.5, regional maps such as AFRICOVER and national maps from mapping agencies and other organizations. The different products are ranked at the national level using crowdsourced data from Geo-Wiki to create a map that reflects the likelihood of cropland. Calibration with national and subnational crop statistics was then undertaken to distribute the cropland within each country and subnational unit. The new IIASA-IFPRI cropland product has been validated using very high-resolution satellite imagery via Geo-Wiki and has an overall accuracy of 82.4%. It has also been compared with the EarthStat cropland Global Change Biology (2015Biology ( ) 21, 1980Biology ( -1992Biology ( , doi: 10.1111 product and shows a lower root mean square error on an independent data set collected from Geo-Wiki. The first ever global field size map was produced at the same resolution as the IIASA-IFPRI cropland map based on interpolation of field size data collected via a Geo-Wiki crowdsourcing campaign. A validation exercise of the global field size map revealed satisfactory agreement with control data, particularly given the relatively modest size of the field size data set used to create the map. Both are critical inputs to global agricultural monitoring in the frame of GEOGLAM and will serve the global land modelling and integrated assessment community, in particular for improving land use models that require baseline cropland information. These products are freely available for downloading from the http://cropland.geo-wiki.org website.

A series of compounds based on the dipeptidyl nitrile scaffold were synthesized and assayed for their inhibitory activity against the T. cruzi cysteine protease cruzain. Structure activity relationships (SARs) were established using three, eleven and twelve variations respectively at the P1, P2 and P3 positions. A K i value of 16 nM was observed for the most potent of these inhibitors which reflects a degree of non-additivity in the SAR. An X-ray crystal structure was determined for the ligand-protein complex for the structural prototype for the series. Twenty three inhibitors were also evaluated for their anti-trypanosomal effects and an EC50 value of 28 μM was observed for the most potent of these. Although there remains scope for further optimization, the knowledge gained from this study is also transferable to the design of cruzain inhibitors based on warheads other than nitrile as well as alternative scaffolds.

A multi-step cascade strategy using integrated ligand- and target-based virtual screening methods was developed to select a small number of compounds from the ZINC database to be evaluated for trypanocidal activity. Winnowing the database to 23 selected compounds, 12 non-covalent binding cruzain inhibitors with affinity values (K i) in the low micromolar range (3–60 µM) acting through a competitive inhibition mechanism were identified. This mechanism has been confirmed by determining the binding mode of the cruzain inhibitor Nequimed176 through X-ray crystallographic studies. Cruzain, a validated therapeutic target for new chemotherapy for Chagas disease, also shares high similarity with the mammalian homolog cathepsin L. Because increased activity of cathepsin L is related to invasive properties and has been linked to metastatic cancer cells, cruzain inhibitors from the same library were assayed against it. Affinity values were in a similar range (4–80 µM), yielding poor selectivity towards cruzain but raising the possibility of investigating such inhibitors for their effect on cell proliferation. In order to select the most promising enzyme inhibitors retaining trypanocidal activity for structure-activity relationship (SAR) studies, the most potent cruzain inhibitors were assayed against T. cruzi-infected cells. Two compounds were found to have trypanocidal activity. Using compound Nequimed42 as precursor, an SAR was established in which the 2-acetamidothiophene-3-carboxamide group was identified as essential for enzyme and parasite inhibition activities. The IC50 value for compound Nequimed42 acting against the trypomastigote form of the Tulahuen lacZ strain was found to be 10.6±0.1 µM, tenfold lower than that obtained for benznidazole, which was taken as positive control. In addition, by employing the strategy of molecular simplification, a smaller compound derived from Nequimed42 with a ligand efficiency (LE) of 0.33 kcal mol−1 atom−1 (compound Nequimed176) is highlighted as a novel non-peptidic, non-covalent cruzain inhibitor as a trypanocidal agent candidate for optimization.

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Food security is a key global concern. By 2050, the global population will exceed 9 billion, and a 50% increase in annual agricultural output will be required to keep up with demand. There are significant additional pressures on existing agricultural land through increased competition from the biofuel sector and the need to elevate feed production, which is being driven by higher levels of meat consumption in low‐ and middle‐income countries.

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Resumo -O objetivo deste trabalho foi estimar e mapear as áreas com as culturas de soja e milho, no Paraná, com uso de imagens multitemporais EVI/Modis. Foram avaliados os anos-safra de 2004/2005 a 2007/2008. Em razão da alta dinâmica temporal e da heterogeneidade de datas de semeadura das culturas no estado, foram utilizadas cenas que contemplavam as fases de pré-plantio e de desenvolvimento inicial das culturas, para gerar a imagem de mínimo EVI (IMIE), e cenas que consideravam o pico vegetativo das culturas, para gerar a imagem de máximo EVI (IMAE). Estas imagens foram utilizadas para gerar a composição colorida RGB (R, IMAE; GB, IMIE), o que permitiu a confecção de máscara das áreas com soja e milho. As estimativas das áreas de máscara por município foram comparadas com dados oficiais de produção agrícola municipal, tendo-se observado bons ajustes (R²>0,84, d>0,95, c>0,85) entre os dados. Para a avaliação da exatidão espacial das máscaras, imagens Landsat-5/TM e AWiFS/IRS foram usadas como referência para construção da matriz de erros. Os resultados obtidos são indicativos de que a metodologia proposta é altamente eficiente e pode ser utilizada para mapeamento dessas culturas.Termos para indexação: classificação de imagens, distribuição espacial de culturas, índice de vegetação, mapeamento, previsão de safras, sensoriamento remoto. Estimation of summer crop areas in the state of Paraná, Brazil, using multitemporal EVI/Modis imagesAbstract -The objective of this work was to estimate and map crop areas with soybean and corn in the state of Paraná, Brazil, using EVI/Modis images. The crop seasons from 2004/2005 to 2007/2008 were evaluated. Due to the high temporal dynamics and difference in sowing dates of the cultures within the state, scenes containing the pre-planting and initial crop development phases were used to obtain the minimum EVI image (IMIE), and scenes at the peak of the crop cycle were used to obtain the maximum EVI image (IMAE). These images were used to generate the RGB color composition (R, IMAE; GB, IMIE), which allowed for the creation of masks of the areas planted with soybean and corn. The estimation of masked areas by municipality was compared with the municipal agricultural production official data, and good fits (R²>0. 84, d>0.95, c>0.85) were observed between data. For spatial accuracy assessment, Landsat-5/TM and AWiFS/IRS images were used as references to build the error matrix. The obtained results indicate that the proposed methodology is highly efficient and may be used as a model for cropland mapping.