A conceptual framework of urban food security and nutrition in low- and middle-income country settings applied to the Asia-Pacific region.

A conceptual framework is presented for enhancing food security and nutrition in urban areas in low- and middle-income countries, highlighting key influencing factors, including food supply chains, community food environments, community infrastructure and services, and numerous underlying individual and household determinants, such as behaviours and dietary practices.

Implications of US agricultural data practices for sustainable food systems research.

Using the tenets of data feminism, we analyse the National Agricultural Statistics Service Quick Stats database - the primary repository of United States agricultural data. We identify unstated assumptions built into the database's scaffolding through data collection, aggregation and dissemination practices, revealing how they facilitate granular analyses of agricultural topics historically judged as national priorities while leaving unilluminated many others of vital importance for contemporary sustainability needs. We argue that this entrenches an inequitable and unsustainable food systems status quo, and we offer recommendations for data providers and users based on principles of reflexivity, context and pluralism.

Design, development, and local production of lipid-based nutritional supplements to enhance the complementary feeding diet: A model for collaboration for a feeding trial in Bangladesh.

: Lipid-based nutrient supplements (LNS) are effective for treating childhood wasting and for preventing stunting, wasting, and anemia, but large-scale production and programmatic use are a barrier. Locally-developed and produced LNS may be more affordable and reduce logistical procurement and importation hurdles, while promoting private sector engagement and partnership. : In northwestern Bangladesh, we conducted a community-based trial of complementary food supplementation to test its efficacy to reduce childhood stunting.

Water in the West: Trends, production efficiency, and a call for open data.

Climate change is projected to transform US agriculture, particularly in places reliant on limited irrigation water resources. As water demand and scarcity increase simultaneously over the coming decades, water managers and growers will need to optimize water use on their irrigated lands. Understanding how growers maintain high yields in arid, water stressed places, while conserving water, is of key importance for the future of US agriculture in the West.

Phenylethyl-substituted pyrimido[2,1-f]purinediones and related compounds: structure-activity relationships as adenosine A(1) and A(2A) receptor ligands.

The synthesis of N-(un)substituted-phenylalkylpyrimido[2,1-f]purinediones was performed starting with 7-(3-chloropropyl)-8-bromotheophylline and 7-(3-chloropropyl)-8-bromo-1,3-dipropylxanthine. Compounds with unsubstituted or substituted ethylene spacer to an aromatic ring were synthesized. Additionally variations in the spacer-elongation of the linker containing more than two atoms, introduction of a double bond or heteroatoms were performed.

N9-benzyl-substituted 1,3-dimethyl- and 1,3-dipropyl-pyrimido[2,1-f]purinediones: synthesis and structure-activity relationships at adenosine A1 and A2A receptors.

Synthesis and physicochemical properties of N-benzyl pyrimido[2,1-f]purinediones are described. These derivatives were synthesized by the cyclization of 7-chloropropylo-8-bromo-1,3-dimethyl- or 1,3-dipropyl xanthine derivatives with corresponding (un)substituted benzylamines. Dipropyl derivatives were obtained under microwave irradiation conditions either.

Improving potency, selectivity, and water solubility of adenosine A1 receptor antagonists: xanthines modified at position 3 and related pyrimido[1,2,3-cd]purinediones.

The structure-activity relationships of xanthine derivatives related to the adenosine A(1) receptor antagonists 8-cyclopentyl-1,3-dipropylxanthine (DPCPX) and 1,3-dipropyl-8-(3-noradamantyl)xanthine (KW3902) were investigated by focusing on variations of the 3-substituent. Aromatic residues were well tolerated by the A(1) receptor in that position. A moderate effect of stereochemistry was found for the 3-(1-phenylethyl)-substituted analogue of DPCPX (S>R) at A(1) and A(3) receptors, whereas the opposite stereoselectivity was observed at the A(2) receptor subtypes.

Synthesis and biological activity of tricyclic aryloimidazo-, pyrimido-, and diazepinopurinediones.

Syntheses and physicochemical properties of N-aryl-substituted imidazo-, pyrimido-, and 1,3-diazepino[2,1-f]purinediones are described. These derivatives were synthesized by the cyclization of 7-haloalkyl-8-bromo-1,3-dimethyl- or 1,3-dipropyl-xanthine derivatives with corresponding arylamines. The obtained compounds (1-40), which can be envisaged as sterically fixed and configurationally stable analogs of 8-styrylxanthines, were evaluated for their affinity to adenosine A(1) and A(2A) receptors, the receptor subtypes that are predominant in the brain.

Tricyclic oxazolo[2,3-f]purinediones: potency as adenosine receptor ligands and anticonvulsants.

Synthesis and physicochemical properties of 7-mono- and 6,7-disubstituted dihydrooxazolo-[3,2-f]purinediones are described. Oxazolo[2,3-f]purinediones were synthesized by cyclization of 8-bromotheophylline with oxiranes. The obtained compounds (1-22) were evaluated for their affinity at adenosine A(1) and A(2A) receptors.

Imidazo[2,1-b]thiazepines: synthesis, structure and evaluation of benzodiazepine receptor binding.

As a continuation of our search for new ligands acting on benzodiazepine receptors among the fused 2-thiohydantoin derivatives, a series of 5-substituted imidazo[2,1-b]thiazepines was synthesized and investigated in radioligand binding studies at the benzodiazepine binding site of GABA(A) receptors in rat brain cortical membranes. Among ortho-substituted 5-arylidene-imidazo[2,1-b]thiazepines compounds could be identified which exhibit affinity for the benzodiazepine binding site at low micromolar concentrations. X-ray structure analyses for two compounds (6ae and 6ag) have been performed.

Pyrimidin-8-on[2,1-f]theophylline-9-alkylcarboxylic acids amides as A1 and A2A adenosine receptor ligands.

Starting from the appropriate esters (1-3), pyrimidin-8-on[2,1-f]theophylline-9-alkylcarboxylic acids amides (4-10) were synthesized and evaluated as hydrochlorides (4a-10a) for their affinity at brain A(1) and A(2A) adenosine receptor subtypes. Radioligand binding assay showed that morpholine-ethyl(-propyl) amide of pyrimidin-8-on[2,1-f]theophylline-9-acetic acid (4a, 5a) exhibited greater affinity and selectivity for A(1) and A(2A) receptors than parent compounds (theophylline and caffeine), with K(i) values: 12.2 and 3.

Impact of the aryl substituent kind and distance from pyrimido[2,1-f]purindiones on the adenosine receptor selectivity and antagonistic properties.

Adenosine receptor (AR) antagonists belong to two major groups of compounds: xanthines and non-xanthines. Recently several annelated xanthine derivatives have been described as selective A(1), A(2A), A(2B) and A(3) ARs antagonists. Contrary to dipropyl derivatives, in the group of dimethyl (un)substituted arylalkyl pyrimido[2,1-f]purindiones selective mainly adenosine A(2A) receptor antagonists were identified.

2-Phenylimidazo[2,1-i]purin-5-ones: structure-activity relationships and characterization of potent and selective inverse agonists at Human A3 adenosine receptors.

Structure-activity relationships of 2-phenyl-imidazo[2,1-i]purin-5-ones as ligands for human A(3) adenosine receptors (ARs) were investigated. An ethyl group in the 8-position of the imidazoline ring of 4-methyl-2-phenyl-imidazopurinone leading to chiral compounds was found to increase affinity for human A(3) ARs by several thousand-fold. Propyl substitution instead of methyl at N4 decreased A(3) affinity but increased A(1) affinity leading to potent A(1)-selective AR antagonists.

Lignans isolated from valerian: identification and characterization of a new olivil derivative with partial agonistic activity at A(1) adenosine receptors.

A methanolic extract of the roots of Valeriana officinalis (valerian) was investigated for its lignan content. In addition to the lignans 8'-hydroxypinoresinol (1) and pinoresinol-4-O-beta-D-glucoside (2), which had already been isolated from valerian in an earlier study, the 7,9'-monoepoxylignans massoniresinol-4'-O-beta-D-glucoside (3), 4'-O-beta-D-glucosyl-9-O-(6' '-deoxysaccharosyl)olivil (4), and berchemol-4'-O-beta-D-glucoside (5) and the 7,9':7',9-diepoxylignans pinoresinol-4,4'-di-beta-O-D-glucoside (6), 8-hydroxypinoresinol-4'-O-beta-D-glucoside (7), and 8'-hydroxypinoresinol-4'-O-beta-D-glucoside (8) were identified. While lignans 3, 6, 7, and 8 had already been isolated from other plants, lignans 4 and 5 are new natural products.

Interactions of valerian extracts and a fixed valerian-hop extract combination with adenosine receptors.

Phytopharmaceuticals and dietary supplements containing valerian are used as mild sleep-inducing agents. An in vitro radioligand binding assay at A(1) and A(2A) adenosine receptors (ARs) was conducted with a fixed extract combination of valerian and hop (Ze 91019) to investigate a possible mechanism for the pharmacological activity of the extract. Component extracts of valerian and hop were also individually investigated.

1,8-disubstituted xanthine derivatives: synthesis of potent A2B-selective adenosine receptor antagonists.

3-Unsubstituted xanthine derivatives bearing a cyclopentyl or a phenyl residue in the 8-position were synthesized and developed as A2B adenosine receptor antagonists. Compounds bearing polar substituents were prepared to obtain water-soluble derivatives. 1-Alkyl-8-phenylxanthine derivatives were found to exhibit high affinity for A2B adenosine receptors (ARs).