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141.
142.
Within the frame of World Health Organisation (WHO) guidelines for the control of soil transmitted helminth (STH) infections, a baseline survey has been conducted in Queimadas Indian schoolchildren (group A) as compared with urban schoolchildren (group B), both located in Ortigueira, Paraná, Brazil, with the aim of orientating investigations. In an opportunistic study, the possible relationship between STH infection and nutritional status has been investigated. A total of 236 schoolchildren aged 5-15 years were enrolled, 100 in group A and 136 in group B. Prevalence of STH infections and heavy intensity infections were significantly higher in the group A (P < .001). A statistical significant correlation between stunting (Z-score < -2) and intensity of STH infections was noted. These results strongly suggested that mass treatment would be indicated in the indigenous community, possibly leading to improved nutritional status. 相似文献
143.
Lee J Reynolds C Jetter MC Youngman MA Hlasta DJ Dax SL Stone DJ Zhang SP Codd EE 《Bioorganic & medicinal chemistry letters》2003,13(11):1879-1882
The design and synthesis of novel pyrrolidine-containing bradykinin antagonists, II, are described. Conformational analysis suggested that a pyrrolidine moiety could substitute for the N-methyl cis-amide moiety of FR 173657. The in vitro binding data showed that the (S)-isomer of II was potent in the bradykinin B(2) receptor-binding assay with a K(i) of 33 nM. The opposite isomer, (R)-II, had a K(i) of 46 nM. The in vitro binding data confirmed our conformational hypothesis. 相似文献
144.
145.
Gomulski LM Torti C Murelli V Bonizzoni M Gasperi G Malacrida AR 《Insect biochemistry and molecular biology》2004,34(2):139-148
The medfly genome has been shown to contain a rich assortment of transposable elements from the mariner, Tc1, hAT and gypsy/Ty3 families. These elements display different levels of diversity, abundance and distribution in the genome. The presence of actively transposing elements in the medfly genome is revealed by hybrid dysgenesis phenomena, insertion site polymorphisms and other genetic instabilities. The medfly has been a target of transformation studies involving the exogenous elements Minos, Hermes and piggyBac from three families. The presence of active endogenous homologous elements can have important implications for the stability of such transgenic lines. The potential applications of endogenous elements for medfly population analysis and control are discussed. 相似文献
146.
McDonnell ME Zhang SP Nasser N Dubin AE Dax SL 《Bioorganic & medicinal chemistry letters》2004,14(2):531-534
A series of structurally simple 7-hydroxynaphthalenyl ureas and amides were discovered to be potent ligands of human vanilloid receptor 1 (VR1). 1-(7-Hydroxynaphthalen-1-yl)-3-(4-trifluoromethylbenzyl)urea 5f exhibited nanomolar binding affinity (K(i)=1.0nM) and upon capsaicin challenge, behaved as a potent functional antagonist (IC(50)=4nM). The synthesis and structure-activity relationships (SARs) for the series are described. 相似文献
147.
Jetter MC Youngman MA McNally JJ Zhang SP Dubin AE Nasser N Dax SL 《Bioorganic & medicinal chemistry letters》2004,14(12):3053-3056
Starting from a low micromolar agonist lead identified by high-throughput screening, series of N-isoquinolin-5-yl-N'-aralkyl ureas and analogous amides were developed as potent antagonists of human vanilloid receptor 1 (VR1). The synthesis and structure-activity relationships (SAR) of the series are described. 相似文献
148.
Gavalda S Braga R Dax C Vigroux A Blonski C 《Bioorganic & medicinal chemistry letters》2005,15(24):5375-5377
Dihydroxyacetone-phosphate and phosphonate derivatives were synthesized bearing a N-sulfonyl hydroxamate moiety. The phosphate derivatives represent competitive inhibitors for the class II-FBP aldolase catalyzed reaction, while the phosphonate isosteres are comparatively weaker inhibitors. 相似文献
149.
150.
Cannon MJ Papalia GA Navratilova I Fisher RJ Roberts LR Worthy KM Stephen AG Marchesini GR Collins EJ Casper D Qiu H Satpaev D Liparoto SF Rice DA Gorshkova II Darling RJ Bennett DB Sekar M Hommema E Liang AM Day ES Inman J Karlicek SM Ullrich SJ Hodges D Chu T Sullivan E Simpson J Rafique A Luginbühl B Westin SN Bynum M Cachia P Li YJ Kao D Neurauter A Wong M Swanson M Myszka DG 《Analytical biochemistry》2004,330(1):98-113
To gauge the experimental variability associated with Biacore analysis, 36 different investigators analyzed a small molecule/enzyme interaction under similar conditions. Acetazolamide (222 g/mol) binding to carbonic anhydrase II (CAII; 30,000 Da) was chosen as a model system. Both reagents were stable and their interaction posed a challenge to measure because of the low molecular weight of the analyte and the fast association rate constant. Each investigator created three different density surfaces of CAII and analyzed an identical dilution series of acetazolamide (ranging from 4.1 to 1000 nM). The greatest variability in the results was observed during the enzyme immobilization step since each investigator provided their own surface activating reagents. Variability in the quality of the acetazolamide binding responses was likely a product of how well the investigators’ instruments had been maintained. To determine the reaction kinetics, the responses from the different density surfaces were fit globally to a 1:1 interaction model that included a term for mass transport. The averaged association and dissociation rate constants were 3.1 ± 1.6 × 106 M−1 s−1 and 6.7 ± 2.5 × 10−2 s−1, respectively, which corresponded to an average equilibrium dissociation constant (KD) of 2.6 ± 1.4 × 10−8 M. The results provide a benchmark of variability in interpreting binding constants from the biosensor and highlight keys areas that should be considered when analyzing small molecule interactions. 相似文献