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Over the years, the energy efficiency of the North American housing stock has significantly improved mainly due to higher insulation levels, more efficient windows and, more importantly, adoption of various energy efficiency measures by building codes. The increased insulation levels of building envelopes for homes leads to a multitude of opportunities as well as challenges. A major opportunity is to reduce heat losses and thereby significantly reducing the space heating loads. However, there are many challenges that necessitate changes in the current construction process, durability of products, and more importantly, the effect of higher insulation levels on the overall moisture performance and expected long-term performance of the building envelope. A major barrier to the uptake of highly insulated homes is the lack of proven evidence of reliable thermal and moisture performance of these homes as might be achieved in various climates of Canada. Following a survey of current construction practices, a set of six wall assemblies with different types of exterior insulation systems were chosen for field monitoring study undertaken in two separate Phases over a two year period in a test facility located in Ottawa, Canada. These wall assemblies ranged from total insulation value of RSI-4.8 to RSI 7.9 (R-27 to R-45). Full scale testing included year-round performance monitoring. These wall specimens were installed in a side-by-side test bay and were subjected to local climate conditions of Ottawa, Canada; on the interior of the specimens conditions were nominally maintained at 20°C and 50% RH. This paper provides results of field trials of the six wall assemblies in terms of their hygrothermal performance and risk for condensation over a two year period of operation., International Conference on Thermal Performance of the Exterior Envelopes of Whole Buildings XIII, 4-8 December, 2016, Clearwater Beach, FL, US

11th Canadian Building Science and Technology Conference: 22 March 2007, Banff, Alberta

Inadequate detailing practice and defective installation of windows has accounted for a significant number of premature failures of the building envelope. This has spurred the development of alternative construction details to manage water intrusion at the wall-window interface. Laboratory investigations focused on assessing the effectiveness of wall-window interface details to manage rainwater intrusion in the wall assembly have provided an effective way to obtain useful information on the varying performance of different interface details. Previous studies undertaken to investigate the effectiveness of details typically used in wood frame low-rise wall assemblies have shown the degree to which different details manage rainwater intrusion and the extent of fault tolerance of these systems. This paper offers a report on more selected results obtained from evaluating the watertightness of a series of four wall-window interface details representative of construction practice across Canada. A brief overview of four sets of wallwindow interface details and variations on their implementation are described in general and details for a set, comprised of two specific wall-window interface details evaluated in the study are provided. The set of two variations of interface details described were configured for a fixed PVC window incorporating mounting flanges and installed in a rainscreen wall. The results of water penetration tests are provided in terms of water entry through deficiencies in the cladding, water collection within the assembly and the severity of the simulated wind-driven rain loads. The effectiveness of the two approaches to window installation in managing rainwater entry is discussed., 11th Canadian Building Science and Technology Conference: 22 March 2007, Banff, Alberta

Recent computer simulation studies at the Institute for Research in Construction (IRC) of the National Research Council (NRC) Canada have indicated that the combined wetting and drying potential of the wood-frame face sealed stucco clad wall is significantly influenced by the water vapour permeability and liquid diffusivity of the stucco material. Lower liquid diffusivity and higher water vapour permeability of the stucco material can positively influence the overall moisture management capacity of the wood-frame face sealed stucco clad wall. This paper presents preliminary experimental results from a pilot research project that aims to use the lessons learned from the simulation studies for the development of new materials or modify existing materials. The results from the experimental study show that it is possible to reduce the water absorption coefficient (a measure of liquid diffusivity) of the stucco material without reducing water vapour permeability through appropriate mix design., 11th Canadian Building Science and Technology Conference: 22 March 2007, Banff, Canada

Inadequate detailing and defective installation of windows has accounted for a significant number of premature failures of the building envelope. This has spurred the development of alternative construction details to control water intrusion at the wall-window interface. However, it is not known how effective these construction details may be over the life expectancy of the wall assembly. Laboratory investigations can provide an effective way to obtain reliable, insightful information regarding the effectiveness of specific wall-window interface details on their ability to influence rainwater entry to the wall assembly. A study was undertaken to investigate the effectiveness of such details typically used in wood frame low-rise wall assemblies to manage rainwater. An overview of the experimental approach and test protocol is given and includes a description of the test apparatus and the basis for estimating the effects on specimenssubjected to simulated climate loads. The test specimen configuration is described and details of specific wall-window interfaces evaluated in the study are provided. Results on water entry for the different wallwindow interface configurations are provided and the effectiveness of different details is discussed., 10th Canadian Conference on Building Science & Technology (10BS&T), May 12, 2005, Ottawa, Ontario, Canada

Several new 2-{[(2E)-3-phenylprop-2-enoyl]amino}benzamides 12a–s and 17t–v were synthesized by stirring in pyridine the (E)-3-(2-R1-3-R2-4-R3-phenyl)acrylic acid chlorides 11c–k and 11t–v with the appropriate anthranilamide derivatives 10a–c or the 5-iodoanthranilic acid 13. Some of the synthesized compounds were evaluated for their in vitro antiproliferative activity against the full NCI tumor cell line panel derived from nine clinically isolated cancer types (leukemia, non-small cell lung, colon, CNS, melanoma, ovarian, renal, prostate and breast). COMPARE analysis, effects on tubulin polymerization in cells and with purified tubulin, and effects on cell cycle distribution for 17t, the most active of the series, indicate that these new antiproliferative compounds act as antitubulin agents.

Recently our research group has reported the synthesis of some 3-amino-N-phenyl-1H-indazole-1-carboxamides able to inhibit at low micromolar concentrations the cell growth of many neoplastic cell lines. The above compounds are unsubstituted in the indazole nucleus and this gives the hope to obtain more active compounds if appropriate substituents are beared by the above nucleus. So, several new N-phenyl-1H-indazole-1-carboxamides 1c-h and 4l,m were prepared by reacting phenyl isocyanates 3a,b with 3-amino-1H-indazoles 2c,e,g, or 1H-indazole 2l respectively. Chemical trasformations of compounds 1a,b and 1g,h gave 3-acetamido-N-phenyl-1H-indazole-1-carboxamides 5a,b, and 3,5-diamino-N-phenyl-1H-indazole-1-carboxamides 4i,j respectively. Finally, 3,5-diacetamido-N-phenyl-1H-indazole-1-carboxamides 6a,b were prepared by acethylation of 4i,j. Some of synthesized compounds were evaluated for their in vitro antiproliferative activity against 60 human tumoral cell lines derived from nine clinically isolated cancer types (leukemia, non-small cell lung, colon, CNS, melanoma, ovarian, renal, prostate and breast). Compound 1c, the most active of the series, was able to inhibit cell growth showing GI50 values in the 0.041-33.6 μM range, being very effective against colon and melanoma cell lines. Compound 1c induced an increase of cells in G0-G1 peak and a decrease of cells in S and G2-M phases when used at a concentration of or higher than 40µM which is the TGI calculated after 24 h of 1c exposure. This could be due to a block of G1-S transition as indicated by the ability of 1c to increase the hypophosphorylate pRb/ total pRb ratio.

Many infections such as otitis media, sinusitis, cholesteatoma, tonsillitis and adenoiditis are caused by biofilm forming mucosal pathogens (P. aeruginosa, S. aureus, S. peneomoniae, H. influenzae and M. catarrhalis). Moreover, the role of biofilms in the chronic otolaryngologic infections has been recognized for otitis media, tonsillitis and rhinosinusitis. Finally, bacterial biofilms of S. aureus, S. epidermis and E. faecalis are the leading cause of medical device-related infections. Pathogens growing as biofilms are intrinsically resistant to conventional antibiotics and therefore the discovery of new compounds able to act against biofilm aggregated micro organisms is an urgent task. Previously, we reported the study on the antibiofilm activity of 4-diazopyrazole derivatives of type 1 against S. aureus ATCC 29213, methycillin-resistant S. aureus ATCC 43866 and methycillin-resistant S. epidermis RP626 preformed biofilms. The compounds were active at the maximum tested concentration of 25 microg/ml. On the basis of these results, we have prepared a new series of 4-diazopyrazole derivatives 2a-i and 3 which take the phenylureido or phenylacetamido moiety at 5-position of the pyrazole nucleus. The compounds has been tested preliminarly against planktonic (single cells) strains of S. aureus (ATCC 25923), S. aureus (ATCC 29213), E. coli (ATCC 25922) and P. aeruginosa (ATCC 9027), showing MIC’s values in the range 50-0.097 microg/ml. Experimental work aimed to verify the effect of the above compounds on the corresponding microbial biofilms are in progress.

A series of new 3-amino-N-phenyl-1H-indazole-1-carboxamides 10 have been prepared from commercially available phenyl isocyanate precursors 8 and 3-aminoindazole 9. Some of the synthesized compounds were evaluated for their in vitro antineoplastic activity against 60 human cell lines derived from seven clinically isolated cancer types (lung, colon, melanoma, renal, ovarian, brain, and leukemia) according to the NCI standard protocol. The test results indicated that 3-amino-1H-indazole-1-carboxamides 10 were endowed with an interesting antiproliferative activity. The most active compounds of this series, 10d,e, were able to inhibit cell growth of many neoplastic cell lines at concentrations lower than 1 μM (0.0153 μM in SR leukemia) causing a block in G0–G1 phase of cell cycle. Analysis of pRb expression showed that these two compounds increased the ratio between underphosphorylated pRb and total pRb. The X-ray structure of 10w, confirmed the 3-amino-N-phenyl-1H-indazole-1-carboxamide structure of compounds 10.

The title compounds were easily synthesized by reacting the 4-aminopyrazole hydrochloride 2 and the substituted 2-nitrobenzoyl chlorides 3a-d. The obtained 2-nitrobenzamides 4a-d were methylated and then reduced to give the corresponding amines 6a-d. These were hydrolyzed then directly converted into 4,10-dihydro-1H-pyrazolo[3,4-c][1,5]benzodiazocine-5,11-diones 1a-d by the action of SOCl2 in benzene. These were tested for their COX inhibitory activity, showing an inhibitory profile against both COX-1 and COX-2, being slightly more selective against COX-2 with a percentage of inhibition, at the concentration of 10 μM, in the range 42.0 – 55.0.

A series of N-1H-indazole-1-carboxamides has been synthesized and their effects on both CDK1/cyclin B and the K-562 (human chronic myelogenus leukemia) cell line were evaluated. Using a computational model, we have observed that all the most active compounds 9e, f, i-n exhibited the same binding mode of purvanalol A in the ATP-binding cleft. Although they were able to moderately inhibit the leukemic cell line K-562 and to show inhibitory activity against the Cdc2-Cyclin B kinase in the low micromolar range, they turned out to be non-cytotoxic against HuDe (IZSL) primary cell cultures from human derm. These preliminary results are quite encouraging in view of the low toxicity demonstrated by the above-mentioned compounds.