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70. SYNTHESIS AND OPIOID RECEPTOR BINDING PROPERTIES OF CONFORMATION-RIGIDIFIED ANALOGUES OF 8-CARBOXAMIDOCYCLAZOCINE AND 8-FORMAMIDOCYCLAZOCINE. Xufeng Sun 1, Mark P. Wentland 1, Robert J. Kucejko 1, and Jean M. Bidlack 2. 1 ; Department of Chemistry and Chemical Biology, Rensselaer Polytechnic Institute, Troy, NY 12180, Fax: 518-276-4887, sunxufeng alum.rpi , 2 ; Department of Pharmacology and Physiology, University of Rochester 8-carboxamidocyclazocine A: X CONH2 ; and 8-formamidocyclazocine A: X NHCHO ; have high binding affinity for mu and kappa opioid receptors. To probe the bioactive conformation of these opiates, rigidified analogues were synthesized. Isoquinolinone B, a ring-closed analogue of 8-carboxamidocyclazocine, showed high affinity for kappa 0.74 nM ; , which is comparable to 8-carboxamidocyclazocine 0.53 nM however, it was less potent for the mu receptor 5.5 vs 0.41 nM ; . Quinolinone C, a ring-closed analogue of 8-formamidocyclazocine, showed very low affinity for both receptors compared to 8-formamidocyclazocine 200 vs 1.9 nM for mu; 100 vs 0.85 nM for kappa ; . These results indicate: 1 ; The bioactive conformation of 8-carboxamidocyclazocine for kappa is similar to the structure of isoquinolinone B. 2 ; The bioactive conformation of 8-carboxamidocyclazocine for mu is different from the structure of isoquinolinone B. 3 ; The bioactive conformation of 8-formamidocyclazocine for both receptors is different from the structure of quinolinone C, for example, trifor lease.
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ICT Penetration and Skills Gap Analysis Report - 2003 The study of the Gap Analysis of ICT Penetration in Egyptian Industries was carried out in three Egyptian industries: ready-made garments, pharmaceutical drug manufacturing and food and beverage industries, all three of which are strategically important Egyptian industries. Drug manufacturing is a strategic socioeconomic sector for the country, producing 92% of the local market needs. Food and Beverage falls within the nation's agricultural sector, which occupies 29% of the nation's workforce and contributes to 16.4% of the nation's annual GDP. Ready-made garments industry, as part of the textiles industry, falls within a national economic sector that accounts for 30% of the nation's workforce and 49% of total Egyptian manufactured goods. All three industries are dynamic exporters.While the three industries analyzed are smaller than the macro-economic sectors in which they are situated, all three themselves, as well as the larger industry contexts in which they are situated, play a vital role in future employment generation, safety, and economic security of the country. All three industries have large, committed corporate players who operate globally through joint ventures, associations and partnerships, as well as on the national market, and a large number of SMEs Small & Medium Enterprises ; as dynamically within regional and international markets, albeit on smaller scales. All three industries will be significantly impacted when the GATT conditions change in 2005. There is little reason to believe that after 2005 Egyptian manufacturing sectors will not experience shake downs, such as what occurred with the Mexican food and beverage SMEs when the NAFTA North American Free Trade Agreement ; went into effect: about 50% of the SMEs in that industry disappeared through their outright failure to compete, much of that failure was attributed to not leveraging ICT for business competitiveness. The findings from the Gap Analysis of IC Penetration in Egyptian Industries show what the current ICT use and needs are in the production, management and growth operations of the three industries. The study also presents important comparative information about how ICT solutions have importantly bolstered the ability of those same industries in other countries similar to Egypt, to compete on international markets and to perform efficiently in their own national markets. The findings in the particular case of Mexico emphatically underscores what the negative impacts on industry can be when it did not leverage the advantages and benefits of ICT for global and national competitiveness and growth. Inversely, when ICT is used to such ends as in the cases of Portugal, France, Argentina, Brazil, and Turkey ; , competitiveness can be raised and growth stimulated. There is openness to learn from these examples, as nearly 100% of the companies in the three industries stated that ICT is "very important" to their business performance and growth. Nonetheless, only 46% of the companies have dedicated ICT budgets 67% of pharmaceuticals; 44% of food and beverage; 27% of ready-made garments ; . This large gap between how ICT is perceived to be important versus what companies are actually doing to strategically address ICT solutions is mainly due to three important factors, for example, tricor 40 mg.
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