We have investigated a series of phenolic diaryl amino piperidine delta opioid receptor agonists, establishing the importance of the phenol functional group and substitution on the piperdine nitrogen for delta agonist activity and selectivity versus the mu and kappa opioid receptors. This study uncovered compounds with improved agonist potency and selectivity compared to the standard, non-peptidic delta agonist SNC-80. In vivo anti-nociceptive activity of analog 8e in two rodent models is discussed, demonstrating the potential of delta agonists to provide a novel mechanism for pain relief.
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| http://dx.doi.org/10.1016/j.bmcl.2009.09.072 | DOI Listing |
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Analytical Chemistry Department, Faculty of Pharmacy, Minia University, Minia, Egypt.
An ecofriendly, effective, and selective spectrofluorimetric approach for natamycin analysis was developed using fluorescamine as a fluorogenic probe. Natamycin is the only topical ocular antifungal medication that is presently on the market for treating keratitis, conjunctivitis, and blepharitis caused by yeast and other fungi. Owing to its primary aliphatic amino group, natamycin can easily interact with fluorescamine resulting in the formation of the highly fluorescent diaryl pyrrolone derivative.
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Laboratorio de Química Inorgánica y Organometálica, Departamento de Química Analítica e Inorgánica, Facultad de Ciencias Químicas, Universidad de Concepción, Edmundo Larenas 129, Casilla 160-C, Concepción 4070386, Chile.
Organic compounds with 1,3-diketone or 3-amino enone functional groups are extremely important as they can be converted into a plethora of carbo- or heterocyclic derivatives or can be used as ligands in the formation of metal complexes. Here, we have achieved the preparation of a series of non-symmetrical β-ketoenamines (O,N,N proligand) of the type (4-MeOCH)C(=O)CH=C(R)NH(Q) obtained through the Schiff base condensation of 1,3-diketones (1-anisoylacetone, 1-anisyl-3-(4-cyanophenyl)-1,3-propanedione, and 1-anisyl-3-(4,4,4-trifluorotolyl)-1,3-propanedione) functionalized with electron donor and electron-withdrawing substituents and 8-aminoquinoline (R = CH, 4-CHCN, 4-CHCF; Q = CHN). Schiff base ketoimines with a pendant quinolyl moiety were isolated as single regioisomers in yields of 22-56% and characterized with FT-IR, H NMR, and UV-visible spectroscopy, as well as single-crystal X-ray crystallography, which allowed for the elucidation of the nature of the isolated regioisomers.
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Department of Chemistry, Dalhousie University, 6274 Coburg Road, P.O. Box 15000, Halifax, Nova Scotia, B3H 4R2, Canada.
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