RESUMO
Soil property and class maps for the continent of Africa were so far only available at very generalised scales, with many countries not mapped at all. Thanks to an increasing quantity and availability of soil samples collected at field point locations by various government and/or NGO funded projects, it is now possible to produce detailed pan-African maps of soil nutrients, including micro-nutrients at fine spatial resolutions. In this paper we describe production of a 30 m resolution Soil Information System of the African continent using, to date, the most comprehensive compilation of soil samples ([Formula: see text]) and Earth Observation data. We produced predictions for soil pH, organic carbon (C) and total nitrogen (N), total carbon, effective Cation Exchange Capacity (eCEC), extractable-phosphorus (P), potassium (K), calcium (Ca), magnesium (Mg), sulfur (S), sodium (Na), iron (Fe), zinc (Zn)-silt, clay and sand, stone content, bulk density and depth to bedrock, at three depths (0, 20 and 50 cm) and using 2-scale 3D Ensemble Machine Learning framework implemented in the mlr (Machine Learning in R) package. As covariate layers we used 250 m resolution (MODIS, PROBA-V and SM2RAIN products), and 30 m resolution (Sentinel-2, Landsat and DTM derivatives) images. Our fivefold spatial Cross-Validation results showed varying accuracy levels ranging from the best performing soil pH (CCC = 0.900) to more poorly predictable extractable phosphorus (CCC = 0.654) and sulphur (CCC = 0.708) and depth to bedrock. Sentinel-2 bands SWIR (B11, B12), NIR (B09, B8A), Landsat SWIR bands, and vertical depth derived from 30 m resolution DTM, were the overall most important 30 m resolution covariates. Climatic data images-SM2RAIN, bioclimatic variables and MODIS Land Surface Temperature-however, remained as the overall most important variables for predicting soil chemical variables at continental scale. This publicly available 30-m Soil Information System of Africa aims at supporting numerous applications, including soil and fertilizer policies and investments, agronomic advice to close yield gaps, environmental programs, or targeting of nutrition interventions.
RESUMO
Food security entails having sufficient, safe, and nutritious food to meet dietary needs. The need to optimise nitrogen (N) use for nutrition security while minimising environmental risks in sub-Saharan Africa (SSA) is overdue. Challenges related to managing N use in SSA can be associated with both insufficient use and excessive loss, and thus the continent must address the 'too little' and 'too much' paradox. Too little N is used in food production (80% of countries have N deficiencies), which has led to chronic food insecurity and malnutrition. Conversely, too much N load in water bodies due mainly to soil erosion, leaching, limited N recovery from wastewater, and atmospheric deposition contributes to eutrophication (152 Gg N year-1 in Lake Victoria, East Africa). Limited research has been conducted to improve N use for food production and adoption remains low, mainly because farming is generally practiced by resource-poor smallholder farmers. In addition, little has been done to effectively address the 'too much' issues, as a consequence of limited research capacity. This research gap must be addressed, and supportive policies operationalised, to maximise N benefits, while also minimising pollution. Innovation platforms involving key stakeholders are required to address N use efficiency along the food supply chain in SSA, as well as other world regions with similar challenges.
RESUMO
Despite investment in programs to manage the development of resistance to existing agents, this continues to drive the need for discovery of novel antiparasitic agents for veterinary medicine. Historically, antiparasitic drug discovery was driven by empirical screening, but technological advances have lead to an increased focus on mechanism-based approaches to drug discovery and this is projected to increase as our capabilities advance to improve both the throughput of assays and the quality of data generated. Investment in the development of combination products with novel agents is increasing and, despite regulatory hurdles in some regions, efforts to globally harmonize regulations will aid in delivering safe, efficacious drugs to help in resistance management and integrated parasite control programs.
Assuntos
Antiparasitários/química , Descoberta de Drogas/tendências , Drogas Veterinárias/química , Aminoacetonitrila/química , Aminoacetonitrila/farmacocinética , Animais , Antiparasitários/farmacocinética , Combinação de Medicamentos , Macrolídeos/química , Macrolídeos/farmacocinética , Oxazinas/química , Oxazinas/farmacocinética , Semicarbazonas/química , Semicarbazonas/farmacocinética , Drogas Veterinárias/farmacocinéticaAssuntos
Budismo/psicologia , Terapia Cognitivo-Comportamental/métodos , Empatia/fisiologia , Transtornos de Enxaqueca/psicologia , Estresse Psicológico/psicologia , Encéfalo/anatomia & histologia , Encéfalo/fisiologia , Terapia Cognitivo-Comportamental/normas , Humanos , Meditação/psicologia , Transtornos de Enxaqueca/etiologia , Transtornos de Enxaqueca/terapia , Transtornos do Humor/prevenção & controle , Transtornos do Humor/psicologia , Transtornos do Humor/terapia , Autoimagem , Psicologia do Self , Comportamento Social , Estresse Psicológico/complicações , Estresse Psicológico/terapiaRESUMO
We describe three novel regioisomeric series of aryl naphthyridine analogs, which are potent antagonists of the Class III GPCR mGlu5 receptor. The synthesis and in vitro and in vivo pharmacological activities of these analogs are discussed.
Assuntos
Naftiridinas/síntese química , Naftiridinas/farmacologia , Receptores de Glutamato Metabotrópico/antagonistas & inibidores , Animais , Células CHO , Cricetinae , Cricetulus , Ratos , Receptor de Glutamato Metabotrópico 5 , Receptores de Glutamato Metabotrópico/fisiologia , Estereoisomerismo , Relação Estrutura-AtividadeRESUMO
A novel series of potent 2-aryl pyrido[2,3-d]pyrimidine mGlu5 receptor antagonists are described. The synthesis and pharmacological activities of these analogs are discussed.
Assuntos
Antagonistas de Aminoácidos Excitatórios/síntese química , Antagonistas de Aminoácidos Excitatórios/farmacologia , Pirimidinas/síntese química , Pirimidinas/farmacologia , Receptores de Glutamato Metabotrópico/antagonistas & inibidores , Animais , Células CHO , Cálcio/metabolismo , Cricetinae , Cricetulus , Inibidores de Ciclo-Oxigenase 2/uso terapêutico , Indicadores e Reagentes , Articulações/patologia , Lactonas/uso terapêutico , Osteoartrite/induzido quimicamente , Osteoartrite/tratamento farmacológico , Osteoartrite/patologia , Piridinas/química , Piridinas/farmacologia , Ratos , Receptor de Glutamato Metabotrópico 5 , Relação Estrutura-Atividade , Sulfonas/uso terapêuticoRESUMO
Rational replacement of the alkyne linker of mGluR5 antagonist MPEP gave 7-arylquinolines. SAR optimization gave an orally active compound with high affinity for the MPEP binding site.
Assuntos
Desenho de Fármacos , Antagonistas de Aminoácidos Excitatórios/química , Antagonistas de Aminoácidos Excitatórios/farmacologia , Quinolinas/química , Quinolinas/farmacologia , Receptores de Glutamato Metabotrópico/antagonistas & inibidores , Modelos Moleculares , Estrutura Molecular , Piridinas/química , Piridinas/farmacologia , Receptor de Glutamato Metabotrópico 5 , Relação Estrutura-AtividadeRESUMO
We describe a series of 2,5 thiazole containing compounds, which are potent antagonists of the integrin alpha(v)beta3 and show selectivity relative to the other integrins, such as alpha(IIb)beta3 and alpha(v)beta6. These analogs were demonstrated to have high bioavailability relative to other relative heterocyclic analogs.
Assuntos
Butiratos/síntese química , Butiratos/farmacocinética , Integrina alfaVbeta3/antagonistas & inibidores , Tiazóis/síntese química , Tiazóis/farmacocinética , Administração Oral , Animais , Antígenos de Neoplasias , Disponibilidade Biológica , Butiratos/administração & dosagem , Cães , Avaliação Pré-Clínica de Medicamentos , Haplorrinos , Integrinas/antagonistas & inibidores , Estrutura Molecular , Complexo Glicoproteico GPIIb-IIIa de Plaquetas/antagonistas & inibidores , Ratos , Relação Estrutura-Atividade , Tiazóis/administração & dosagemRESUMO
We describe a series of 1,2,4-oxadiazoles, which are potent antagonists of the integrin alpha(v)beta3 and, in addition, show selectivity relative to the other beta3 integrin alpha(IIb)beta3. In whole cells, the majority of these analogs also demonstrated modest selectivity against other alpha(v) integrins such as alpha(v)beta1 and alpha(v)beta6.
Assuntos
Butiratos/síntese química , Butiratos/farmacologia , Integrina alfaVbeta3/antagonistas & inibidores , Oxidiazóis/síntese química , Oxidiazóis/farmacologia , Antígenos de Neoplasias , Butiratos/química , Linhagem Celular , Humanos , Integrinas/antagonistas & inibidores , Estrutura Molecular , Oxidiazóis/química , Receptores de Vitronectina/antagonistas & inibidores , Relação Estrutura-AtividadeRESUMO
[reaction: see text] The total synthesis of (+)-sparteine was accomplished from 2,5-norbornadione in 15 steps and 15.7% overall yield. The key steps were two ring-expansion reactions, one involving an intramolecular Schmidt reaction and one using a novel variant of the photo-Beckmann rearrangement.