Stereoselective synthesis of a MCHr1 antagonist

Melanin-concentrating hormone (MCH) is implicated in the feeding behavior in mammals affording a potential target to control overeating in people. Compound 1 (AMG 076) has been identified as a potent MCHr1 antagonist for the treatment of obesity. A synthesis suitable for the large-scale preparation of this lead candidate was developed to support preclinical studies. A Robinson annulation of benzylpiperidone and resolution of the desired enone from a mixture of the diastereomers afforded key intermediate 6 after a stereoselective hydrogenation. Subsequent Fischer indole synthesis with hydrazine 5 then provided the advanced intermediate, indole 2. Two complementary reductive amination strategies employing either aldehyde 3 or lactol 4 led to the synthesis of title compound 1.     

New features in the class of association models

The most common association models are the U-, R-, C- and RC-models, achieved when only one dimension on the association is considered as significant (M = 1). Whenever more than one dimensions are significant (M > 1), the only kind of association assumed for each dimension is of the RC-type with the exception of Goodman's R + C + RC, R + RC, C + RC, U + RC and R + C models. Extending the idea of U-, R-, and C-models to association models with M > 1, relaxing the equidistance principle for successive categories for the known scores and using orthogonal polynomials, some new models are developed. Two classical sets of data are used to illustrate the advantages of the newly introduced models. Comparisons in terms of chi-square goodness of fit indicate that some of the newly introduced models perform better than the models fitted so far on these data sets. © 1998 John Wiley & Sons, Ltd.     

Transgenic Artemisia dubia WALL showed altered phytochemistry and pharmacology

The rol genes have been shown to enhance the production of secondary metabolites in plants. This report examines the effect of trans-genes (rol ABC) on possible high production of biologically important phytochemicals and enhanced pharmacological activities. Three transgenic lines (1, 2 and 3) of Artemisia dubia WALL (transformed with Agrobacterium tumefaciens harboring rol ABC genes) were subjected to phytochemical analysis and pharmacological studies. A great variation in phytochemistry and the pharmacological activities was observed not only between the transgenic and non-transgenic control plants but also among the transgenic lines itself. Comparative chemical profile obtained via HPLC, TLC and spectrophotometry showed high degree of variations in the quantity of phytochemicals. An increased production of total flavonoids (71.1% in transgenic line 2) and total phenolics (110.8% in transgenic line 1), increase in caffeic acid and catechin and a decrease in gallic acid content in the extracts of transformed plants compared to the untransformed control plants was decreased. In case of pharmacological activities, moderate to high level increase in antimicrobial (antibacterial and antifungal) activities, cytotoxicity (14.1%), antitumor (29%) and antioxidant activities (23.9%) was observed (in transgenic line 2). In general all the three transgenic lines under study showed improvement in their pharmacological activities in the order of transgenic line 2 > 1 > 3 > control. The implication of these findings will help to meet the increasing demand of pharmacologically important compounds.     

Generalized holographic dark energy model

In this paper, the model of the holographic Chaplygin gas has been extended to two general cases: first the case of a modified variable Chaplygin gas and second the case of the viscous generalized Chaplygin gas. The dynamics of the model is expressed by the use of scalar fields and scalar potentials.     

Optimizing distortion for real‐time data gathering in randomly deployed sensor networks

In several wireless sensor network applications, it is required to perform real‐time reconstruction of the data field being sensed by the network. This task is generally carried out at a central location, e.g. sink node, using a continuous data gathering phase and relying on the known correlation properties of the underlying data field. Estimating the overall spatial and temporal distortion in the reconstructed field is an important step toward deciding the number of sensors to be deployed and the data collection algorithm to be used. However, estimating distortion in arbitrary networks is a challenging task. Existing work has focused on regular network deployments such as one‐ and two‐dimensional girds. Such deployments are deemed infeasible in a realistic environment. In this paper, we consider one‐ and two‐dimensional random networks. For the analysis purposes, we assume that the nodes are randomly deployed following Poisson distribution. We determine the total distortion function given the correlation coefficients of the field while assuming a simple data gathering protocol. Based on this, we also determine the optimal number of nodes to be deployed in the field that will minimize distortion. Copyright © 2009 John Wiley & Sons, Ltd.     

A mild,efficient and selective iodination of aromatic compounds using iodine and 1,4-bis(triphenylphosphonium)-2-butene peroxodisulfate

A simple and efficient method for the iodination of aromatic compounds has been achieved in the presence of iodine and 1,4-bis(triphenylphosphonium)-2-butene peroxodisulfate.     

On the commutativity degree of compact groups

In any finite group G, the commutativity degree of G (denoted by d(G)) is the probability that two randomly chosen elements of G commute. More generally, for every n ≥ 2 the nth commutativity degree (denoted by d _n (G)) is the probability that a randomly chosen ordered (n + 1)-tuple of the group elements is mutually commuting. The aim of this paper is to generalize the definition of d(G) and d _n (G) to every compact group G (infinite and even uncountable). We shall state some results concerning compact groups and we will extend some results in Erfanian et al. (Comm. Algebra 35 (2007), 4183–4197) and Lescot (J. Algebra 177 (1995), 847–869).     

Fixed point for set-valued mappings satisfying an implicit relation in partially ordered metric spaces

Let (X,?) be a partially ordered set and d be a complete metric on X. Let F,G be two set-valued mappings on X. We obtained sufficient conditions for the existence of common fixed point of F and G satisfying an implicit relation in partially ordered set X.     

Surface-directed boundary flow in microfluidic channels

Channel geometry combined with surface chemistry enables a stable liquid boundary flow to be attained along the surfaces of a 12 microm diameter hydrophilic glass fiber in a closed semi-elliptical channel. Surface free energies and triangular corners formed by PDMS/glass fiber or OTS/glass fiber surfaces are shown to be responsible for the experimentally observed wetting phenomena and formation of liquid boundary layers that are 20-50 microm wide and 12 microm high. Viewing this stream through a 20 microm slit results in a virtual optical window with a 5 pL liquid volume suitable for cell counting and pathogen detection. The geometry that leads to the boundary layer is a closed channel that forms triangular corners where glass fiber and the OTS coated glass slide or PDMS touch. The contact angles and surfaces direct positioning of the fluid next to the fiber. Preferential wetting of corner regions initiates the boundary flow, while the elliptical cross-section of the channel stabilizes the microfluidic flow. The Young-Laplace equation, solved using fluid dynamic simulation software, shows contact angles that exceed 105 degrees will direct the aqueous fluid to a boundary layer next to a hydrophilic fiber with a contact angle of 5 degrees. We believe this is the first time that an explanation has been offered for the case of a boundary layer formation in a closed channel directed by a triangular geometry with two hydrophobic wetting edges adjacent to a hydrophilic surface.