Investigation of the SAR lead (methoxyalkyl)thiazole 1-[3-(naphth-2-ylmethoxy)phenyl]-1-thiazol-2-ylprop yl methyl ether (1, ICI 211965) led to methoxytetrahydropyrans, a new series 5-lipoxygenase (5-LPO) inhibitors exemplified by parent compound 4-[3-(naphth-2-ylmethoxy)phenyl]-4- methoxy-3,4,5,6-tetrahydro-2H-pyran (4f). In vitro 4f inhibited leukotriene C4 (LTC4) synthesis in zymosan-stimulated plasma-free mouse macrophages and LTB4 A-23187-stimulated human whole blood (IC50s 0.5 nM 0.07...

ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTIndazolinones, a new series of redox-active 5-lipoxygenase inhibitors with built-in selectivity and oral activityP. Bruneau, C. Delvare, M. P. Edwards, R. McMillanCite this: J. Med. Chem. 1991, 34, 3, 1028–1036Publication Date (Print):March 1, 1991Publication History Published online1 May 2002Published inissue 1 March 1991https://pubs.acs.org/doi/10.1021/jm00107a023https://doi.org/10.1021/jm00107a023research-articleACS PublicationsRequest reuse...

Because of their impact on hydraulic structure design as well floodplain management, flood quantiles must be estimated with the highest precision given available information. If site interest has been monitored for a sufficiently long period (more than 30–40 years), at‐site frequency analysis can used to estimate fair precision. Otherwise, regional estimation may mitigate lack data, but local information is then ignored. A commonly approach combine and linear empirical Bayes estimation:...

ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXT(Methoxyalkyl)thiazoles: a new series of potent, selective, and orally active 5-lipoxygenase inhibitors displaying high enantioselectivityT. Geoffrey C. Bird, Pierre Bruneau, Graham Crawley, Martin P. Edwards, Stephen J. Foster, Jean Marc Girodeau, John F. Kingston, Rodger M. McMillanCite this: Med. Chem. 1991, 34, 7, 2176–2186Publication Date (Print):July 1, 1991Publication History Published online1 May 2002Published inissue 1 July...

Abstract In this article, an approach using residual kriging (RK) in physiographical space is proposed for regional flood frequency analysis. The constructed physiographical/climatic characteristics of gauging basins by means canonical correlation analysis (CCA). This a modified version the original method, based on ordinary (OK). It intended to handle effectively any possible spatial trends within hydrological variables over space. approach, trend first quantified and removed from variable...

This paper describes the pharmacological profile of ICI207968, a novel, orally‐active and selective inhibitor 5‐lipoxygenase. Inhibition leukotriene B 4 (LTB ) synthesis by 2‐substituted indazolinones was not directly related to redox potential but critically dependent on nature N2 substituent. 2‐(3‐Pyridylmethyl)‐indazolinone (ICI207968) combined selectivity oral potency. In several in vitro systems ICI207968 exhibited similar lipoxygenase inhibitory potency (IC 50 values from 1.5 μ m 6.0...

This paper presents artificial neural network (ANN) models designed to predict ice in Canadian lakes and reservoirs during the early winter thickness growth period. The fit measurements at one or more monitored period either same locations for dates without (local ANN models) any site region (regional model), provided that required meteorological input variables are available. were selected after preliminary assessments adapted from time series of daily mean air temperature, rainfall, cloud...

With rising shares of photovoltaic (PV) generated electricity in the power grids, PV forecasting is rapidly gaining importance for energy suppliers and grid operators. But specifically, distribution system operators (DSOs) require detailed forecasts at higher spatial resolutions, to manage congestions avoid voltage band violations, which are local phenomena. In view future smart operation, authors propose a scheme using numerical weather prediction (NWP) data feed performance model compute...

Floods, as extreme hydrological phenomena, can be described by more than one correlated characteristic, such peak, volume and duration. These characteristics should jointly considered since they are generally not independent. For an ungauged site, univariate regional flood frequency analysis (FA) provides a limited assessment of events. A recent study proposed procedure for FA in multivariate framework. This represents version the index-flood model is based on copulas quantiles. The...

Twitter has significant potential as a source of Volunteered Geographic Information (VGI), its content is updated at high frequency, with availability thanks to dedicated interfaces. However, the diversity types and low average accuracy geographic information attached individual tweets remain obstacles in this context. The contributions paper relate general goal extracting actionable regarding impact natural hazards on specific region from social platforms, such Twitter. Specifically, our...

L'estimation de l'intensité précipitations extrêmes est un sujet recherche en pleine expansion. Nous présentons ici une synthèse des travaux sur l'analyse régionale précipitations. Les principales étapes revues sont les méthodes d'établissement régions homogènes, la sélection fonctions distributions régionales et l'ajustement paramètres ces fonctions. De nombreux s'inspirent l'approche développée régionalisation crues. types indice crues ont été utilisées par plusieurs auteurs. homogènes...

This work describes and evaluates a novel interactive visual clustering system. It combines 2D projection with algorithm that operates on this projected data. Users can interact directly through the representation, by providing examples according to their expert ground truth. Each interaction incrementally updates associated clustering. Experiments show effectiveness of method, as few one leading tangible influence visualization.

This paper proposes a technique for simplifying given Gaussian mixture model, i.e. reformulating the density in more parcimonious manner, if possible (less components mixture). Numerous applications requiring aggregation of models from various sources, or index structures over sets fast access, may benefit technique. Variational Bayesian estimation mixtures is known to be powerful on punctual data. We derive herein new version variational-Bayes EM algorithm that operates and suppresses...

Finding the optimal number of groups in context a clustering algorithm is identified as difficult problem. In this article, we automate choice for spectral with novel heuristic. Our method deterministic, and remarkable by its low computational burden. We show effectiveness respect to state art, further investigate assumptions underlying previous work through an empirical study, support synthetic real data sets.