Toward a simplified measure of asthma severity for applied research |
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Authors: | DR Wahlgren MF Hovell GE Matt SB Meltzer JM Zakarian EO Meltzer |
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Affiliation: | Medicinal Chemistry, Universidad de Navarra, Pamplona, Spain. |
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Abstract: | The synthesis and preliminary evaluation of new benzof]quinoline and pyridine derivatives, obtained by application of the Reissert method and its modifications, as HIV-1 RT inhibitors and anti-infectives are presented. The most active products against HIV-1 RT wild type are the ethyl 2-cyano-1,2-dihydrobenzof]quinoline-1-carboxylate 2b, propyl 2-cyano-1,2-dihydrobenzof]quinoline-1-carboxylate 2c, and 2-cyano-1-(2'-furoyl)-1,2-dihydrobenzof]quinoline 2n, which maintain their activity against the mutant type P236L, resulting inactive against the Y181C type. Using the data previously obtained by our research team for analogous series derived from quinoline as reference, the compounds which have now been obtained present an increase in the cytotoxic character attributable to the introduction of a benzene ring fused with the quinoline base nucleus, as well as a decrease of the activity as HIV-1 RT inhibitors when the quinoline benzenic ring is eliminated. |
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